메뉴 건너뛰기




Volumn , Issue , 2008, Pages 103-166

Drug discovery: From hits to clinical candidates

Author keywords

[No Author keywords available]

Indexed keywords


EID: 84883705157     PISSN: None     EISSN: None     Source Type: Book    
DOI: None     Document Type: Chapter
Times cited : (19)

References (304)
  • 1
    • 33646442687 scopus 로고    scopus 로고
    • Recent progress in histamine H3 receptor chemistry
    • Aslanian, R. and Shih, N.Y. 2004. Recent progress in histamine H3 receptor chemistry. Ann. Rep. Med. Chem. 39: 57-66.
    • (2004) Ann. Rep. Med. Chem. , vol.39 , pp. 57-66
    • Aslanian, R.1    Shih, N.Y.2
  • 2
    • 6444235896 scopus 로고    scopus 로고
    • Medicinal chemical and pharmacological aspects of imidazole-containing histamine H3 receptor antagonists
    • Stark, H., Kathmann, M., Schlicker, E. et al. 2004. Medicinal chemical and pharmacological aspects of imidazole-containing histamine H3 receptor antagonists. Mini-Rev. Med. Chem. 4: 965-977.
    • (2004) Mini-Rev. Med. Chem. , vol.4 , pp. 965-977
    • Stark, H.1    Kathmann, M.2    Schlicker, E.3
  • 4
    • 4944229347 scopus 로고    scopus 로고
    • Medicinal chemistry and biological properties of non-imidazole histamine H3 antagonists
    • Cowart, M., Altenbach, R., Black, L. et al. 2004. Medicinal chemistry and biological properties of non-imidazole histamine H3 antagonists. Mini-Rev. Med. Chem. 4: 979-992.
    • (2004) Mini-Rev. Med. Chem. , vol.4 , pp. 979-992
    • Cowart, M.1    Altenbach, R.2    Black, L.3
  • 5
    • 14044275765 scopus 로고    scopus 로고
    • The histamine H3 receptor: From gene cloning to H3 receptor drugs
    • Leurs, R., Bakker, R.A., Timmerman, H. et al. 2005. The histamine H3 receptor: From gene cloning to H3 receptor drugs. Nat. Rev. Drug Disc. 4: 107-120.
    • (2005) Nat. Rev. Drug Disc. , vol.4 , pp. 107-120
    • Leurs, R.1    Bakker, R.A.2    Timmerman, H.3
  • 6
    • 29144437722 scopus 로고    scopus 로고
    • Keynote review: Histamine H3 receptor antagonists reach out for the clinic
    • Celanire, S., Wijtmans, M., Talaga, P. et al. 2005. Keynote review: Histamine H3 receptor antagonists reach out for the clinic. Drug Disc. Today 10: 1613-1627.
    • (2005) Drug Disc. Today , vol.10 , pp. 1613-1627
    • Celanire, S.1    Wijtmans, M.2    Talaga, P.3
  • 7
    • 33646369637 scopus 로고    scopus 로고
    • Recent medicinal chemistry of the histamine H3 receptor
    • Letavic, M.A., Barbier, A.J., Dvorak, C.A. et al. 2006. Recent medicinal chemistry of the histamine H3 receptor. Prog. Med. Chem. 44: 181-206.
    • (2006) Prog. Med. Chem. , vol.44 , pp. 181-206
    • Letavic, M.A.1    Barbier, A.J.2    Dvorak, C.A.3
  • 8
    • 85057702554 scopus 로고    scopus 로고
    • Thomson Current Drugs. Thomson Scientific
    • IDdb3. 2007. Investigational Drugs Database (IDdb). Thomson Current Drugs. Thomson Scientific. http://www. iddb3.com.
    • (2007) Investigational Drugs Database (IDdb)
  • 10
    • 0034047202 scopus 로고    scopus 로고
    • Cloning of rat histamine H3 receptor reveals distinct species pharmacological profiles
    • Lovenberg, T.W., Pyati, J., Chang, H. et al. 2000. Cloning of rat histamine H3 receptor reveals distinct species pharmacological profiles. J. Pharmacol. Exp. Ther. 293: 771-778.
    • (2000) J. Pharmacol. Exp. Ther. , vol.293 , pp. 771-778
    • Lovenberg, T.W.1    Pyati, J.2    Chang, H.3
  • 11
    • 34447276432 scopus 로고    scopus 로고
    • Recent advances in the development of histamine H3 antagonists
    • Berlin, M. and Boyce, C.W. 2007. Recent advances in the development of histamine H3 antagonists. Expert Opin. Ther. Pat. 17: 675-687.
    • (2007) Expert Opin. Ther. Pat. , vol.17 , pp. 675-687
    • Berlin, M.1    Boyce, C.W.2
  • 12
    • 84944482644 scopus 로고
    • The physiological action of beta-iminazolylethylamine
    • Dale, H. and Laidlaw, P. 1910. The physiological action of beta-iminazolylethylamine. J. Physiol. 41: 318-344.
    • (1910) J. Physiol. , vol.41 , pp. 318-344
    • Dale, H.1    Laidlaw, P.2
  • 13
    • 33644853786 scopus 로고    scopus 로고
    • Naturally occurring and synthetic imidazoles: Their chemistry and their biological activities
    • De Luca, L. 2006. Naturally occurring and synthetic imidazoles: Their chemistry and their biological activities. Curr. Med. Chem. 13: 1-23.
    • (2006) Curr. Med. Chem. , vol.13 , pp. 1-23
    • De Luca, L.1
  • 14
    • 0035804954 scopus 로고    scopus 로고
    • Approaches to the synthesis of some tyrosine-derived marine sponge metabolites: Synthesis of verongamine and purealidin N
    • Boehlow, T.R., Harburn, J.J., and Spilling, C.D. 2001. Approaches to the synthesis of some tyrosine-derived marine sponge metabolites: Synthesis of verongamine and purealidin N. J. Org. Chem. 66: 3111-3118.
    • (2001) J. Org. Chem. , vol.66 , pp. 3111-3118
    • Boehlow, T.R.1    Harburn, J.J.2    Spilling, C.D.3
  • 15
    • 8744283471 scopus 로고    scopus 로고
    • Pharmacological effects of carcinine on histaminergic neurons in the brain
    • Chen, Z., Sakurai, E., Hu, W. et al. 2004. Pharmacological effects of carcinine on histaminergic neurons in the brain. Br. J. Pharmacol. 143: 573-580.
    • (2004) Br. J. Pharmacol. , vol.143 , pp. 573-580
    • Chen, Z.1    Sakurai, E.2    Hu, W.3
  • 16
    • 12344275459 scopus 로고    scopus 로고
    • Dose-dependent effects of l-carnosine on the renal sympathetic nerve and blood pressure in urethane-anesthetized rats
    • Tanida, M., Niijima, A., Fukuda, Y. et al. 2005. Dose-dependent effects of l-carnosine on the renal sympathetic nerve and blood pressure in urethane-anesthetized rats. Am. J. Physiol. 288: R447-R455.
    • (2005) Am. J. Physiol. , vol.288 , pp. R447-R455
    • Tanida, M.1    Niijima, A.2    Fukuda, Y.3
  • 17
    • 33846543219 scopus 로고    scopus 로고
    • Carnosine protects against NMDA-induced neurotoxicity in differentiated rat PC12 cells through carnosine-histidine-histamine pathway and H1/H3 receptors
    • Shen, Y., Hu, W.W., Fan, Y.Y. et al. 2007. Carnosine protects against NMDA-induced neurotoxicity in differentiated rat PC12 cells through carnosine-histidine-histamine pathway and H1/H3 receptors. Biochem. Pharmacol. 73: 709-717.
    • (2007) Biochem. Pharmacol. , vol.73 , pp. 709-717
    • Shen, Y.1    Hu, W.W.2    Fan, Y.Y.3
  • 18
    • 0242525249 scopus 로고    scopus 로고
    • Possible role of l-carnosine in the regulation of blood glucose through controlling autonomic nerves
    • Nagai, K., Niijima, A., Yamano, T. et al. 2003. Possible role of l-carnosine in the regulation of blood glucose through controlling autonomic nerves. Exp. Biol. Med. 228: 1138-1145.
    • (2003) Exp. Biol. Med. , vol.228 , pp. 1138-1145
    • Nagai, K.1    Niijima, A.2    Yamano, T.3
  • 19
    • 0028172783 scopus 로고
    • L-Carnosine (β-alanyl-l-histidine) and carcinine (β-alanylhistamine) act as natural antioxidants with hydroxyl-radicalscavenging and lipid-peroxidase activities
    • Babizhayev, M., Seguin, M., Gueyene, J. et al. 1994. l-Carnosine (β-alanyl-l-histidine) and carcinine (β-alanylhistamine) act as natural antioxidants with hydroxyl-radicalscavenging and lipid-peroxidase activities. Biochemistry 304: 509-516.
    • (1994) Biochemistry , vol.304 , pp. 509-516
    • Babizhayev, M.1    Seguin, M.2    Gueyene, J.3
  • 21
    • 30344458497 scopus 로고    scopus 로고
    • Aplysamine-1 and related analogs as histamine H3 receptor antagonists
    • Swanson, D.M., Wilson, S.J., Boggs, J.D. et al. 2006. Aplysamine-1 and related analogs as histamine H3 receptor antagonists. Bioorg. Med. Chem. Lett. 16: 897-900.
    • (2006) Bioorg. Med. Chem. Lett. , vol.16 , pp. 897-900
    • Swanson, D.M.1    Wilson, S.J.2    Boggs, J.D.3
  • 22
    • 85057687773 scopus 로고    scopus 로고
    • Discovery of novel natural alkaloid conessine as potent histamine H3 receptor antagonist
    • Washington, DC, August 28 to September 1, 2005. Abst. MEDI-104
    • Zhao, C., Bennani, Y.L., Gopalakrishnan, S. et al. 2005. Discovery of novel natural alkaloid conessine as potent histamine H3 receptor antagonist, 230th ACS National Meeting, Washington, DC, August 28 to September 1, 2005. Abst. MEDI-104.
    • (2005) 230th ACS National Meeting
    • Zhao, C.1    Bennani, Y.L.2    Gopalakrishnan, S.3
  • 25
    • 0029999489 scopus 로고    scopus 로고
    • An asymmetric route to the conanine BCDE ring system. A formal total synthesis of (+)-conessine
    • Kopach, M.E., Fray, A.H., and Meyers, A.I. 1996. An asymmetric route to the conanine BCDE ring system. A formal total synthesis of (+)-conessine. J. Am. Chem. Soc. 118: 9876-9883.
    • (1996) J. Am. Chem. Soc. , vol.118 , pp. 9876-9883
    • Kopach, M.E.1    Fray, A.H.2    Meyers, A.I.3
  • 26
    • 3342941927 scopus 로고    scopus 로고
    • Highly enantioselective construction of fused pyrrolidine systems that contain a quarternary stereocenter: Concise formal synthesis of (+)-conessine
    • Jiang, B. and Xu, M. 2004. Highly enantioselective construction of fused pyrrolidine systems that contain a quarternary stereocenter: Concise formal synthesis of (+)-conessine. Angew. Chem. Int. Ed. 43: 2543-2546.
    • (2004) Angew. Chem. Int. Ed. , vol.43 , pp. 2543-2546
    • Jiang, B.1    Xu, M.2
  • 27
    • 33749042117 scopus 로고    scopus 로고
    • Drug-induced phospholipidosis
    • Anderson, N. and Borlak, J. 2006. Drug-induced phospholipidosis. FEBS Lett. 580: 5533-5540.
    • (2006) FEBS Lett. , vol.580 , pp. 5533-5540
    • Anderson, N.1    Borlak, J.2
  • 28
    • 0035687129 scopus 로고    scopus 로고
    • Drug-induced phospholipidosis: Are there functional consequences
    • Reasor, M.J. and Kacew, S. 2001. Drug-induced phospholipidosis: Are there functional consequences. Exp. Biol. Med. 226: 825-830.
    • (2001) Exp. Biol. Med. , vol.226 , pp. 825-830
    • Reasor, M.J.1    Kacew, S.2
  • 29
    • 18144424791 scopus 로고    scopus 로고
    • Isolation, characterization and antiplasmodial activity of steroidal alkaloids from Funtumia elastica (Preuss) Stapf
    • Zirihi, G.N., Grellier, P., Guede-Guina, F. et al. 2005. Isolation, characterization and antiplasmodial activity of steroidal alkaloids from Funtumia elastica (Preuss) Stapf. Bioorg. Med. Chem. Lett. 15: 2637-2640.
    • (2005) Bioorg. Med. Chem. Lett. , vol.15 , pp. 2637-2640
    • Zirihi, G.N.1    Grellier, P.2    Guede-Guina, F.3
  • 30
    • 0042844744 scopus 로고    scopus 로고
    • Natural products as source of new drugs over the period 1981-2002
    • Newman, D.J., Cragg, C.G., and Snader, K.M. 2003. Natural products as source of new drugs over the period 1981-2002. J. Nat. Prod. 66: 1022-1037.
    • (2003) J. Nat. Prod. , vol.66 , pp. 1022-1037
    • Newman, D.J.1    Cragg, C.G.2    Snader, K.M.3
  • 31
    • 0020587209 scopus 로고
    • Autoinhibition of brain histamine release mediated by a novel class (H3) of histamine receptor
    • Arrang, J.M., Garbarg, M., and Schwartz, J.C. 1983. Autoinhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. Nature 302: 832-837.
    • (1983) Nature , vol.302 , pp. 832-837
    • Arrang, J.M.1    Garbarg, M.2    Schwartz, J.C.3
  • 32
    • 23944433719 scopus 로고    scopus 로고
    • Evaluation of histamine H1-, H2-, and H3- re ceptor ligands at the human histamine H4 receptor: Identification of 4-methylhistamine as the first potent and selective H4 receptor agonist
    • Lim, H.D., van Rijn, R.M., Ling, P. et al. 2005. Evaluation of histamine H1-, H2-, and H3- re ceptor ligands at the human histamine H4 receptor: Identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J. Pharmacol. Exp. Ther. 314: 1310-1321.
    • (2005) J. Pharmacol. Exp. Ther. , vol.314 , pp. 1310-1321
    • Lim, H.D.1    van Rijn, R.M.2    Ling, P.3
  • 33
    • 33645551062 scopus 로고    scopus 로고
    • Compared pharmacology of human histamine H3 and H4 receptors: Structure-activity relationships of histamine derivatives
    • Gbahou, F., Vincent, L., Humbert-Claude, M. et al. 2006. Compared pharmacology of human histamine H3 and H4 receptors: Structure-activity relationships of histamine derivatives. Br. J. Pharmacol. 147: 744-754.
    • (2006) Br. J. Pharmacol. , vol.147 , pp. 744-754
    • Gbahou, F.1    Vincent, L.2    Humbert-Claude, M.3
  • 34
    • 10744234014 scopus 로고    scopus 로고
    • Synthesis and structure- activity relationships of conformationally constrained histamine H3 receptor agonists
    • Kitbunnadaj, R., Zuiderveld, O.P., De Esch, I.J.P. et al. 2003. Synthesis and structure- activity relationships of conformationally constrained histamine H3 receptor agonists. J. Med. Chem. 46: 5445-5457.
    • (2003) J. Med. Chem. , vol.46 , pp. 5445-5457
    • Kitbunnadaj, R.1    Zuiderveld, O.P.2    De Esch, I.J.P.3
  • 35
    • 0141940125 scopus 로고    scopus 로고
    • Synthesis of (+-)-trans- or cis-(5-amino methyltetrahydrofuranyl)imidazole by Mitsunobu cyclization: Synthetic studies toward novel histamine H3 or H4-ligands
    • Harusawa, S., Araki, L., Imazu, T. et al. 2003. Synthesis of (+-)-trans- or cis-(5-amino methyltetrahydrofuranyl)imidazole by Mitsunobu cyclization: Synthetic studies toward novel histamine H3 or H4-ligands. Chem. Pharm. Bull. 51: 325-329.
    • (2003) Chem. Pharm. Bull. , vol.51 , pp. 325-329
    • Harusawa, S.1    Araki, L.2    Imazu, T.3
  • 36
    • 20144385213 scopus 로고    scopus 로고
    • N-Substituted piperidinyl alkyl imidazoles: Discovery of methimepip as a potent and selective histamine H3 receptor agonist
    • Kitbunnadaj, R., Hashimoto, T., Poli, E. et al. 2005. N-Substituted piperidinyl alkyl imidazoles: Discovery of methimepip as a potent and selective histamine H3 receptor agonist. J. Med. Chem. 48: 2100-2107.
    • (2005) J. Med. Chem. , vol.48 , pp. 2100-2107
    • Kitbunnadaj, R.1    Hashimoto, T.2    Poli, E.3
  • 37
    • 27544465179 scopus 로고    scopus 로고
    • New high affinity H3 receptor agonists without a basic side chain
    • Kitbunnadaj, R., Hoffmann, M., Fratantoni, S.A. et al. 2005. New high affinity H3 receptor agonists without a basic side chain. Bioorg. Med. Chem. 13: 6309-6323.
    • (2005) Bioorg. Med. Chem. , vol.13 , pp. 6309-6323
    • Kitbunnadaj, R.1    Hoffmann, M.2    Fratantoni, S.A.3
  • 38
    • 0038644592 scopus 로고    scopus 로고
    • Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-Aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure
    • Kazuta, Y., Hirano, K., Natsume, K. et al. 2003. Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-Aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure. J. Med. Chem. 46: 1980-1988.
    • (2003) J. Med. Chem. , vol.46 , pp. 1980-1988
    • Kazuta, Y.1    Hirano, K.2    Natsume, K.3
  • 39
    • 2342470022 scopus 로고    scopus 로고
    • Identification of 4-(1HImidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H3 receptor agonist
    • Kitbunnadaj, R., Zuiderveld, O.P., Christophe, B. et al. 2004. Identification of 4-(1HImidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H3 receptor agonist. J. Med. Chem. 47: 2414-2417.
    • (2004) J. Med. Chem. , vol.47 , pp. 2414-2417
    • Kitbunnadaj, R.1    Zuiderveld, O.P.2    Christophe, B.3
  • 40
    • 85057672114 scopus 로고    scopus 로고
    • Pharmacological characterization, in vitro and in vivo ADME properties of immethridine, a potent and highly selective histamine H3R agonist
    • Delphi, Greece, Abst. P5
    • Celanire, S., Gillard, M., Christophe, B. et al. 2007. Pharmacological characterization, in vitro and in vivo ADME properties of immethridine, a potent and highly selective histamine H3R agonist. 35th Eur. Histamine Res. Soc. Delphi, Greece, Abst. P5.
    • (2007) 35th Eur. Histamine Res. Soc.
    • Celanire, S.1    Gillard, M.2    Christophe, B.3
  • 41
    • 33646119663 scopus 로고    scopus 로고
    • A chemical switch for the modulation of the functional activity of higher homologues of histamine on the human histamine H3 receptor: Effect of various substitutions at the primary amino function
    • Govoni, M., Lim, H.D., El Atmioui, D. et al. 2006. A chemical switch for the modulation of the functional activity of higher homologues of histamine on the human histamine H3 receptor: Effect of various substitutions at the primary amino function. J. Med. Chem. 49: 2549-2557.
    • (2006) J. Med. Chem. , vol.49 , pp. 2549-2557
    • Govoni, M.1    Lim, H.D.2    El Atmioui, D.3
  • 42
    • 0034866384 scopus 로고    scopus 로고
    • Azomethine prodrugs of (R)-a-methylhistamine, a highly potent and selective histamine H3-receptor agonist
    • Krause, M., Stark, H., Schunack, W. 2001. Azomethine prodrugs of (R)-a-methylhistamine, a highly potent and selective histamine H3-receptor agonist. Curr. Med. Chem. 8: 1329-1340.
    • (2001) Curr. Med. Chem. , vol.8 , pp. 1329-1340
    • Krause, M.1    Stark, H.2    Schunack, W.3
  • 44
    • 0035191953 scopus 로고    scopus 로고
    • Enzyme-catalyzed prodrug approaches for the histamine H3-receptor agonist (R)-a-methylhistamine
    • Stark, H., Krause, M., Rouleau, A. et al. 2001. Enzyme-catalyzed prodrug approaches for the histamine H3-receptor agonist (R)-a-methylhistamine. Bioorg. Med. Chem. Lett. 9: 191-198.
    • (2001) Bioorg. Med. Chem. Lett. , vol.9 , pp. 191-198
    • Stark, H.1    Krause, M.2    Rouleau, A.3
  • 45
    • 0037194643 scopus 로고    scopus 로고
    • Influence of bulky substituents on histamine H3 receptor agonist/antagonist properties
    • Sasse, A., Ligneau, X., Rouleau, A. et al. 2002. Influence of bulky substituents on histamine H3 receptor agonist/antagonist properties. J. Med. Chem. 45: 4000-4010.
    • (2002) J. Med. Chem. , vol.45 , pp. 4000-4010
    • Sasse, A.1    Ligneau, X.2    Rouleau, A.3
  • 46
    • 18544405824 scopus 로고    scopus 로고
    • Meta-substituted aryl(thio)ethers as potent partial agonists (or antagonists) for the histamine H3 receptor lacking a nitrogen atom in the side chain
    • Pelloux-Leon, N., Fkyerat, A., Piripitsi, A. et al. 2004. Meta-substituted aryl(thio)ethers as potent partial agonists (or antagonists) for the histamine H3 receptor lacking a nitrogen atom in the side chain. J. Med. Chem. 47: 3264-3274.
    • (2004) J. Med. Chem. , vol.47 , pp. 3264-3274
    • Pelloux-Leon, N.1    Fkyerat, A.2    Piripitsi, A.3
  • 47
    • 2342503894 scopus 로고    scopus 로고
    • 4-(w-(Alkyloxy)alkyl)-1H-imidazole derivatives as histamine H3 receptor antagonists/agonists
    • Meier, G., Krause, M., Huels, A. et al. 2004. 4-(w-(Alkyloxy)alkyl)-1H-imidazole derivatives as histamine H3 receptor antagonists/agonists. J. Med. Chem. 47: 2678-2687.
    • (2004) J. Med. Chem. , vol.47 , pp. 2678-2687
    • Meier, G.1    Krause, M.2    Huels, A.3
  • 48
    • 0031854957 scopus 로고    scopus 로고
    • High antagonist potency of GT-2227 and GT-2331, new histamine H3 receptor antagonists, in two functional models
    • Tedford, C.E., Hoffmann, M., Seyedi, N. et al. 1998. High antagonist potency of GT-2227 and GT-2331, new histamine H3 receptor antagonists, in two functional models. Eur. J. Pharmacol. 351: 307-311.
    • (1998) Eur. J. Pharmacol. , vol.351 , pp. 307-311
    • Tedford, C.E.1    Hoffmann, M.2    Seyedi, N.3
  • 49
    • 0346100541 scopus 로고    scopus 로고
    • An efficient multigram synthesis of the potent histamine H3 antagonist GT-2331 and the reassessment of the absolute configuration
    • Liu, H., Kerdesky, F.A., Black, L.A. et al. 2004. An efficient multigram synthesis of the potent histamine H3 antagonist GT-2331 and the reassessment of the absolute configuration. J. Org. Chem. 69: 192-194.
    • (2004) J. Org. Chem. , vol.69 , pp. 192-194
    • Liu, H.1    Kerdesky, F.A.2    Black, L.A.3
  • 50
    • 29344433472 scopus 로고    scopus 로고
    • Detailed pharmacological characterization of GT-2331 for the rat histamine H3 receptor
    • Ito, S., Yoshimoto, R., Miyamoto, Y. et al. 2006. Detailed pharmacological characterization of GT-2331 for the rat histamine H3 receptor. Eur. J. Pharmacol. 529: 40-46.
    • (2006) Eur. J. Pharmacol. , vol.529 , pp. 40-46
    • Ito, S.1    Yoshimoto, R.2    Miyamoto, Y.3
  • 51
    • 0034649481 scopus 로고    scopus 로고
    • High constitutive activity of native H3 receptors regulates histamine neurons in brain
    • Morisset, S., Rouleau, A., Lineau, X. et al. 2000. High constitutive activity of native H3 receptors regulates histamine neurons in brain. Nature 408: 860-864.
    • (2000) Nature , vol.408 , pp. 860-864
    • Morisset, S.1    Rouleau, A.2    Lineau, X.3
  • 52
    • 0141702358 scopus 로고    scopus 로고
    • Protean agonism at histamine H3 receptors in vitro and in vivo
    • Gbahou, F., Rouleau, A., Morisset, S. et al. 2003. Protean agonism at histamine H3 receptors in vitro and in vivo. Proc. Natl Acad. Sci. U.S.A. 100: 11086-11091.
    • (2003) Proc. Natl Acad. Sci. U.S.A. , vol.100 , pp. 11086-11091
    • Gbahou, F.1    Rouleau, A.2    Morisset, S.3
  • 53
    • 0035083109 scopus 로고    scopus 로고
    • Inverse, protean, and ligand-selective agonism: Matters of receptor conformation
    • Kenakin, T. 2001. Inverse, protean, and ligand-selective agonism: Matters of receptor conformation. FASEB J. 15: 598-611.
    • (2001) FASEB J. , vol.15 , pp. 598-611
    • Kenakin, T.1
  • 54
    • 4344659412 scopus 로고    scopus 로고
    • Turning from monogamy to strategic promiscuity
    • Stark, H. 2004. Turning from monogamy to strategic promiscuity. Drug Disc. Today 9: 736-737.
    • (2004) Drug Disc. Today , vol.9 , pp. 736-737
    • Stark, H.1
  • 55
    • 23944456700 scopus 로고    scopus 로고
    • The histamine H4 receptor as a new therapeutic target for inflammation
    • De Esch, I.J.P., Thurmond, R.L., Jongejan, A. et al. 2005. The histamine H4 receptor as a new therapeutic target for inflammation. Trends Pharmacol. Sci. 26: 462-469.
    • (2005) Trends Pharmacol. Sci. , vol.26 , pp. 462-469
    • De Esch, I.J.P.1    Thurmond, R.L.2    Jongejan, A.3
  • 56
    • 21144450185 scopus 로고    scopus 로고
    • Lack of cataleptogenic potentiation with non-imidazole H3 receptor antagonists reveals potential drug-drug interactions between imidazole-based H3 receptor antagonists and antipsychotic drugs
    • Zhang, M., Ballard, M.E., Pan, L. et al. 2005. Lack of cataleptogenic potentiation with non-imidazole H3 receptor antagonists reveals potential drug-drug interactions between imidazole-based H3 receptor antagonists and antipsychotic drugs. Brain Res. 1045: 142-149.
    • (2005) Brain Res. , vol.1045 , pp. 142-149
    • Zhang, M.1    Ballard, M.E.2    Pan, L.3
  • 57
    • 0036025401 scopus 로고    scopus 로고
    • Coordination of histamine H3 receptor antagonists with human adrenal cytochrome P450 enzymes
    • Yang, R., Hey, J.A., Aslanian, R. et al. 2002. Coordination of histamine H3 receptor antagonists with human adrenal cytochrome P450 enzymes. Pharmacology 66: 128-135.
    • (2002) Pharmacology , vol.66 , pp. 128-135
    • Yang, R.1    Hey, J.A.2    Aslanian, R.3
  • 58
    • 33748547737 scopus 로고    scopus 로고
    • Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure
    • Watanabe, M., Kazuta, Y., Hayashi, H. et al. 2006. Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure. J. Med. Chem. 49: 5587-5596.
    • (2006) J. Med. Chem. , vol.49 , pp. 5587-5596
    • Watanabe, M.1    Kazuta, Y.2    Hayashi, H.3
  • 59
    • 27944437327 scopus 로고    scopus 로고
    • Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold
    • Vaccaro, W.D., Sher, R., Berlin, M. et al. 2006. Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold. Bioorg. Med. Chem. Lett. 16: 395-399.
    • (2006) Bioorg. Med. Chem. Lett. , vol.16 , pp. 395-399
    • Vaccaro, W.D.1    Sher, R.2    Berlin, M.3
  • 60
    • 30344443374 scopus 로고    scopus 로고
    • Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl]piperidine series of histamine H3 receptor antagonists
    • Berlin, M., Ting, P.C., Vaccaro, W.D. et al. 2006. Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl]piperidine series of histamine H3 receptor antagonists. Bioorg. Med. Chem. Lett. 16: 989-994.
    • (2006) Bioorg. Med. Chem. Lett. , vol.16 , pp. 989-994
    • Berlin, M.1    Ting, P.C.2    Vaccaro, W.D.3
  • 61
    • 38849194032 scopus 로고    scopus 로고
    • Synthesis and stability in biological of 1Himidazole-1-carboxylates of RS203, an antagonist of the histamine H3 receptor
    • Rivara, M., Vacondio, F., Silva, C. et al. 2008. Synthesis and stability in biological of 1Himidazole-1-carboxylates of RS203, an antagonist of the histamine H3 receptor. Chem. Biodivers. 5: 140-152.
    • (2008) Chem. Biodivers. , vol.5 , pp. 140-152
    • Rivara, M.1    Vacondio, F.2    Silva, C.3
  • 62
    • 0031794361 scopus 로고    scopus 로고
    • Inhibition and induction of cytochrome P450 and the clinical implications
    • Lin, J.H. and Lu, A.Y. 1998. Inhibition and induction of cytochrome P450 and the clinical implications. Clin. Pharmacokinet. 35: 361-390.
    • (1998) Clin. Pharmacokinet. , vol.35 , pp. 361-390
    • Lin, J.H.1    Lu, A.Y.2
  • 63
    • 0037101814 scopus 로고    scopus 로고
    • Ciproxifan, a histamine H3-receptor antagonist/inverse agonist, potentiates neurochemical and behavioral effects of haloperidol in the rat
    • Pillot, C., Ortiz, J., Heron, A. et al. 2002. Ciproxifan, a histamine H3-receptor antagonist/inverse agonist, potentiates neurochemical and behavioral effects of haloperidol in the rat. J. Neuroscience 22: 7272-7280.
    • (2002) J. Neuroscience , vol.22 , pp. 7272-7280
    • Pillot, C.1    Ortiz, J.2    Heron, A.3
  • 70
    • 0034990158 scopus 로고    scopus 로고
    • Influence of imidazole replacement in different structural classes of histamine H3-receptor antagonists
    • Meier, G., Apelt, J., Reichert, U. et al. 2001. Influence of imidazole replacement in different structural classes of histamine H3-receptor antagonists. Eur. J. Pharm. Sci. 13: 249-259.
    • (2001) Eur. J. Pharm. Sci. , vol.13 , pp. 249-259
    • Meier, G.1    Apelt, J.2    Reichert, U.3
  • 71
    • 33947289522 scopus 로고    scopus 로고
    • Brain histamine and schizophrenia: Potential therapeutic applications of H3-receptor inverse agonists studied with BF2.649
    • Ligneau, X., Landais, L., Perrin, D. et al. 2007. Brain histamine and schizophrenia: Potential therapeutic applications of H3-receptor inverse agonists studied with BF2.649. Biochem. Pharmacol. 73: 1215-1224.
    • (2007) Biochem. Pharmacol. , vol.73 , pp. 1215-1224
    • Ligneau, X.1    Landais, L.2    Perrin, D.3
  • 72
    • 33845904178 scopus 로고    scopus 로고
    • BF2.649 [1-{3-[3-(4-chlorophenyl)pro poxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: Preclinical pharmacology
    • Ligneau, X., Perrin, D., Landais, L. et al. 2007. BF2.649 [1-{3-[3-(4-chlorophenyl)pro poxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: Preclinical pharmacology. J. Pharmacol. Exp. Ther. 320: 365-375.
    • (2007) J. Pharmacol. Exp. Ther. , vol.320 , pp. 365-375
    • Ligneau, X.1    Perrin, D.2    Landais, L.3
  • 73
    • 22044446536 scopus 로고    scopus 로고
    • Piperidine-containing histamine H3 receptor antagonists of the carbamate series: The alkyl derivatives
    • Lazewska, D., Kiec-Kononowicz, K., Elz, S. et al. 2005. Piperidine-containing histamine H3 receptor antagonists of the carbamate series: The alkyl derivatives. Pharmazie 60: 403-410.
    • (2005) Pharmazie , vol.60 , pp. 403-410
    • Lazewska, D.1    Kiec-Kononowicz, K.2    Elz, S.3
  • 74
    • 33645900260 scopus 로고    scopus 로고
    • Ether derivatives of 3-piperidinopropan-1-ol as non-imidazole histamine H3 receptor antagonists
    • Lazewska, D., Ligneau, X., Schwartz, J.C. et al. 2006. Ether derivatives of 3-piperidinopropan-1-ol as non-imidazole histamine H3 receptor antagonists. Bioorg. Med. Chem. 14: 3522-3529.
    • (2006) Bioorg. Med. Chem. , vol.14 , pp. 3522-3529
    • Lazewska, D.1    Ligneau, X.2    Schwartz, J.C.3
  • 75
    • 0242417538 scopus 로고    scopus 로고
    • Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(Phenoxymethyl)benzyl)piperidines and related compounds
    • Miko, T., Ligneau, X., Pertz, H.H. et al. 2003. Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(Phenoxymethyl)benzyl)piperidines and related compounds. J. Med. Chem. 46: 1523-1530.
    • (2003) J. Med. Chem. , vol.46 , pp. 1523-1530
    • Miko, T.1    Ligneau, X.2    Pertz, H.H.3
  • 76
    • 2142768757 scopus 로고    scopus 로고
    • Structural variations of 1-(4-(phenoxymethyl) benzyl)piperidines as nonimidazole histamine H3 receptor antagonists
    • Miko, T., Ligneau, X., Pertz, H.H. et al. 2004. Structural variations of 1-(4-(phenoxymethyl) benzyl)piperidines as nonimidazole histamine H3 receptor antagonists. Bioorg. Med. Chem. 12: 2727-2736.
    • (2004) Bioorg. Med. Chem. , vol.12 , pp. 2727-2736
    • Miko, T.1    Ligneau, X.2    Pertz, H.H.3
  • 77
    • 33846614652 scopus 로고    scopus 로고
    • In vitro pharmacology at human histamine H3 receptors and brain access of non-imidazole alkylpiperidine derivatives
    • Bertoni, S., Flammini, L., Manenti, V. et al. 2007. In vitro pharmacology at human histamine H3 receptors and brain access of non-imidazole alkylpiperidine derivatives. Pharmacol. Res. 55: 111-116.
    • (2007) Pharmacol. Res. , vol.55 , pp. 111-116
    • Bertoni, S.1    Flammini, L.2    Manenti, V.3
  • 79
    • 33947119591 scopus 로고    scopus 로고
    • Histamine H3 receptor antagonists: From target identification to drug leads
    • Bonaventure, P., Letavic, M., Dugovic, C. et al. 2007. Histamine H3 receptor antagonists: From target identification to drug leads. Biochem. Pharmacol. 73: 1084-1096.
    • (2007) Biochem. Pharmacol. , vol.73 , pp. 1084-1096
    • Bonaventure, P.1    Letavic, M.2    Dugovic, C.3
  • 80
    • 0023792442 scopus 로고
    • Synthesis of (aryloxy)alkylamines. 2. Novel imidazo-fused heterocycles with calcium channel blocking and local anesthetic activity
    • Sanfilippo, P.J., Urbanski, M., Press, J.B. et al. 1988. Synthesis of (aryloxy)alkylamines. 2. Novel imidazo-fused heterocycles with calcium channel blocking and local anesthetic activity. J. Med. Chem. 31: 2221-2227.
    • (1988) J. Med. Chem. , vol.31 , pp. 2221-2227
    • Sanfilippo, P.J.1    Urbanski, M.2    Press, J.B.3
  • 82
    • 0038702085 scopus 로고    scopus 로고
    • Non-imidazole heterocyclic histamine H3 receptor antagonists
    • Chai, W., Breitenbucher, J.G., Kwok, A. et al. 2003. Non-imidazole heterocyclic histamine H3 receptor antagonists. Bioorg. Med. Chem. Lett. 13: 1767-1770.
    • (2003) Bioorg. Med. Chem. Lett. , vol.13 , pp. 1767-1770
    • Chai, W.1    Breitenbucher, J.G.2    Kwok, A.3
  • 85
    • 0041418310 scopus 로고    scopus 로고
    • A new class of diamine-based human histamine H3 receptor antagonists: 4-(Aminoalkoxy)benzylamines
    • Apodaca, R., Dvorak, C.A., Xiao, W. et al. 2003. A new class of diamine-based human histamine H3 receptor antagonists: 4-(Aminoalkoxy)benzylamines. J. Med. Chem. 46: 3938-3944.
    • (2003) J. Med. Chem. , vol.46 , pp. 3938-3944
    • Apodaca, R.1    Dvorak, C.A.2    Xiao, W.3
  • 87
    • 33747352284 scopus 로고    scopus 로고
    • Radiosynthesis and biodistribution of a histamine H3 receptor antagonist 4-[3-(4-piperidin-1-yl-but-1- ynyl)-[11C]benzyl]-morpholine: Evaluation of a potential PET ligand
    • Airaksinen, A.J., Jablonowski, J.A., van der Mey, M. et al. 2006. Radiosynthesis and biodistribution of a histamine H3 receptor antagonist 4-[3-(4-piperidin-1-yl-but-1- ynyl)-[11C]benzyl]-morpholine: Evaluation of a potential PET ligand. Nucl. Med. Biol. 33: 801-810.
    • (2006) Nucl. Med. Biol. , vol.33 , pp. 801-810
    • Airaksinen, A.J.1    Jablonowski, J.A.2    van der Mey, M.3
  • 90
    • 15444363211 scopus 로고    scopus 로고
    • 4-phenoxypiperidines: Potent, conformationally restricted, non-imidazole histamine H3 antagonists
    • Dvorak, C.A., Apodaca, R., Barbier, A.J. et al. 2005. 4-phenoxypiperidines: Potent, conformationally restricted, non-imidazole histamine H3 antagonists. J. Med. Chem. 48: 2229-2238.
    • (2005) J. Med. Chem , vol.48 , pp. 2229-2238
    • Dvorak, C.A.1    Apodaca, R.2    Barbier, A.J.3
  • 96
    • 8644269592 scopus 로고    scopus 로고
    • A scalable synthesis of a histamine H3 receptor antagonist
    • Mani, N.S., Jablonowski, J.A., and Jones, T.K. 2004. A scalable synthesis of a histamine H3 receptor antagonist. J. Org. Chem. 69: 8115-8117.
    • (2004) J. Org. Chem. , vol.69 , pp. 8115-8117
    • Mani, N.S.1    Jablonowski, J.A.2    Jones, T.K.3
  • 97
    • 33644834851 scopus 로고    scopus 로고
    • The challenge of drug discovery of a GPCR target: Analysis of preclinical pharmacology of histamine H3 antagonists/inverse agonists
    • Hancock, A.A. 2006. The challenge of drug discovery of a GPCR target: Analysis of preclinical pharmacology of histamine H3 antagonists/inverse agonists. Biochem. Pharmacol. 71: 1103-1113.
    • (2006) Biochem. Pharmacol. , vol.71 , pp. 1103-1113
    • Hancock, A.A.1
  • 98
    • 33645287272 scopus 로고    scopus 로고
    • Histamine H3 receptor antagonists: Preclinical promise for treating obesity and cognitive disorders
    • Esbenshade, T.A., Fox, G.B., and Cowart, M.D. 2006. Histamine H3 receptor antagonists: Preclinical promise for treating obesity and cognitive disorders. Mol. Interv. 6: 77-88, 59.
    • (2006) Mol. Interv. , vol.6
    • Esbenshade, T.A.1    Fox, G.B.2    Cowart, M.D.3
  • 100
    • 0037025462 scopus 로고    scopus 로고
    • Structure-activity relationships of nonimidazole H(3) receptor ligands. Part 1
    • Faghih, R., Dwight, W., Gentles, R. et al. 2002. Structure-activity relationships of nonimidazole H(3) receptor ligands. Part 1. Bioorg. Med. Chem. Lett. 12: 2031-2034.
    • (2002) Bioorg. Med. Chem. Lett. , vol.12 , pp. 2031-2034
    • Faghih, R.1    Dwight, W.2    Gentles, R.3
  • 101
    • 0037025466 scopus 로고    scopus 로고
    • Structure-activity relationships of nonimidazole H3 receptor ligands. Part 2: Binding preference for d-amino acids motifs
    • Faghih, R., Dwight, W., Black, L. et al. 2002. Structure-activity relationships of nonimidazole H3 receptor ligands. Part 2: Binding preference for d-amino acids motifs. Bioorg. Med. Chem. Lett. 12: 2035-2037.
    • (2002) Bioorg. Med. Chem. Lett. , vol.12 , pp. 2035-2037
    • Faghih, R.1    Dwight, W.2    Black, L.3
  • 102
    • 0037648479 scopus 로고    scopus 로고
    • Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects
    • Esbenshade, T.A., Krueger, K.M., Miller, T.R. et al. 2003. Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects. J. Pharmacol. Exp. Ther. 305: 887-896.
    • (2003) J. Pharmacol. Exp. Ther. , vol.305 , pp. 887-896
    • Esbenshade, T.A.1    Krueger, K.M.2    Miller, T.R.3
  • 103
    • 0038662678 scopus 로고    scopus 로고
    • Two novel and selective nonimidazole H3 receptor antagonists A-304121 and A-317920: II. In vivo behavioral and neurophysiological characterization
    • Fox, G.B., Pan, J.B., Radek, R.J. et al. 2003. Two novel and selective nonimidazole H3 receptor antagonists A-304121 and A-317920: II. In vivo behavioral and neurophysiological characterization. J. Pharmacol. Exp. Ther. 305: 897-908.
    • (2003) J. Pharmacol. Exp. Ther. , vol.305 , pp. 897-908
    • Fox, G.B.1    Pan, J.B.2    Radek, R.J.3
  • 104
    • 18644364402 scopus 로고    scopus 로고
    • Synthesis and evaluation of potent pyrrolidine H3 antagonists
    • Vasudevan, A., Conner, S.E., Gentles, R.G. et al. 2002. Synthesis and evaluation of potent pyrrolidine H3 antagonists. Bioorg. Med. Chem. Lett. 12: 3055-3058.
    • (2002) Bioorg. Med. Chem. Lett. , vol.12 , pp. 3055-3058
    • Vasudevan, A.1    Conner, S.E.2    Gentles, R.G.3
  • 106
    • 1642534334 scopus 로고    scopus 로고
    • Structure-activity relationships of non-imidazole H3 receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists
    • Gfesser, G.A., Zhang, H., Dinges, J. et al. 2004. Structure-activity relationships of non-imidazole H3 receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists. Bioorg. Med. Chem. Lett. 14: 673-676.
    • (2004) Bioorg. Med. Chem. Lett. , vol.14 , pp. 673-676
    • Gfesser, G.A.1    Zhang, H.2    Dinges, J.3
  • 107
    • 18144373094 scopus 로고    scopus 로고
    • Structure-activity relationships of arylbenzofuran H3 receptor antagonists
    • Gfesser, G.A., Faghih, R., Bennani, Y.L. et al. 2005. Structure-activity relationships of arylbenzofuran H3 receptor antagonists. Bioorg. Med. Chem. Lett. 15: 2559-2563.
    • (2005) Bioorg. Med. Chem. Lett. , vol.15 , pp. 2559-2563
    • Gfesser, G.A.1    Faghih, R.2    Bennani, Y.L.3
  • 108
    • 4544303028 scopus 로고    scopus 로고
    • D-amino acid homopiperazine amides: Discovery of A-320436, a potent and selective non-imidazole histamine H(3)-receptor antagonist
    • Curtis, M.P., Dwight, W., Pratt, J. et al. 2004. D-amino acid homopiperazine amides: Discovery of A-320436, a potent and selective non-imidazole histamine H(3)-receptor antagonist. Arch. Pharm. 337: 219-229.
    • (2004) Arch. Pharm. , vol.337 , pp. 219-229
    • Curtis, M.P.1    Dwight, W.2    Pratt, J.3
  • 110
    • 1642353566 scopus 로고    scopus 로고
    • Histamine H3 antagonists in models of obesity
    • Hancock, A.A., Bush, E.N., Jacobson, P.B. et al. 2004. Histamine H3 antagonists in models of obesity. Inflamm. Res. 53: S47-S48.
    • (2004) Inflamm. Res. , vol.53 , pp. S47-S48
    • Hancock, A.A.1    Bush, E.N.2    Jacobson, P.B.3
  • 111
    • 12144289304 scopus 로고    scopus 로고
    • Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist
    • Hancock, A.A., Bennani, Y.L., Bush, E.N. et al. 2004. Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist. Eur. J. Pharmacol. 487: 183-197.
    • (2004) Eur. J. Pharmacol. , vol.487 , pp. 183-197
    • Hancock, A.A.1    Bennani, Y.L.2    Bush, E.N.3
  • 112
    • 21144456878 scopus 로고    scopus 로고
    • Antiobesity evaluation of histamine H3 receptor (H3R) antagonist analogs of A-331440 with improved safety and efficacy
    • Hancock, A.A., Diehl, M.S., Fey, T.A. et al. 2005. Antiobesity evaluation of histamine H3 receptor (H3R) antagonist analogs of A-331440 with improved safety and efficacy. Inflamm. Res. 54: S27-S29.
    • (2005) Inflamm. Res. , vol.54 , pp. S27-S29
    • Hancock, A.A.1    Diehl, M.S.2    Fey, T.A.3
  • 113
    • 17144380866 scopus 로고    scopus 로고
    • Assessment of pharmacology and potential antiobesity properties of H3 receptor antagonists/inverse agonists
    • Hancock, A.A. and Brune, M.E. 2005. Assessment of pharmacology and potential antiobesity properties of H3 receptor antagonists/inverse agonists. Expert Opin. Invest. Drugs 14: 223-241.
    • (2005) Expert Opin. Invest. Drugs , vol.14 , pp. 223-241
    • Hancock, A.A.1    Brune, M.E.2
  • 114
    • 33646798771 scopus 로고    scopus 로고
    • Distinctions and contradistinctions between antiobesity histamine H3 receptor (H3R) antagonists compared to cognition-enhancing H3 receptor antagonists
    • Hancock, A.A., Bitner, R.S., Krueger, K.M. et al. 2006. Distinctions and contradistinctions between antiobesity histamine H3 receptor (H3R) antagonists compared to cognition-enhancing H3 receptor antagonists. Inflamm. Res. 55: S42-S44.
    • (2006) Inflamm. Res. , vol.55 , pp. S42-S44
    • Hancock, A.A.1    Bitner, R.S.2    Krueger, K.M.3
  • 115
    • 4944261888 scopus 로고    scopus 로고
    • In vitro optimization of structure activity relationships of analogs of A-331440 combining radioligand receptor binding assays and micronucleus assays of potential antiobesity histamine H3 receptor antagonists
    • Hancock, A.A., Diehl, M.S., Faghih, R. et al. 2004. In vitro optimization of structure activity relationships of analogs of A-331440 combining radioligand receptor binding assays and micronucleus assays of potential antiobesity histamine H3 receptor antagonists. Basic Clin. Pharmacol. Tox. 95: 144-152.
    • (2004) Basic Clin. Pharmacol. Tox. , vol.95 , pp. 144-152
    • Hancock, A.A.1    Diehl, M.S.2    Faghih, R.3
  • 116
    • 85057708412 scopus 로고    scopus 로고
    • Effects of A-423579, a novel histamine-3 receptor antagonist in rodent models of diet-induced obesity
    • Washington, DC, April 17-21. Abst. #394.5
    • Fey, T.A., Bush, E.A., Dickinson, R.A. et al. 2004. Effects of A-423579, a novel histamine-3 receptor antagonist in rodent models of diet-induced obesity. Experimental Biology, Washington, DC, April 17-21. Abst. #394.5.
    • (2004) Experimental Biology
    • Fey, T.A.1    Bush, E.A.2    Dickinson, R.A.3
  • 118
    • 0037424719 scopus 로고    scopus 로고
    • Synthesis and SAR of aminoalkoxybiaryl-4-carboxamides: Novel and selective histamine H3 receptor antagonists
    • Faghih, R., Dwight, W., Pan, J.B. et al. 2003. Synthesis and SAR of aminoalkoxybiaryl-4-carboxamides: Novel and selective histamine H3 receptor antagonists. Bioorg. Med. Chem. Lett. 13: 1325-1328.
    • (2003) Bioorg. Med. Chem. Lett. , vol.13 , pp. 1325-1328
    • Faghih, R.1    Dwight, W.2    Pan, J.B.3
  • 119
    • 3843054587 scopus 로고    scopus 로고
    • Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist
    • Esbenshade, T.A., Fox, G.B., Krueger, K.M. et al. 2004. Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist. Biochem. Pharmacol. 68: 933-945.
    • (2004) Biochem. Pharmacol. , vol.68 , pp. 933-945
    • Esbenshade, T.A.1    Fox, G.B.2    Krueger, K.M.3
  • 120
    • 1642299838 scopus 로고    scopus 로고
    • The medicinal chemistry of novel H(3) antagonists
    • Cowart, M., Faghih, R., Gfesser, G. et al. 2004. The medicinal chemistry of novel H(3) antagonists. Inflamm. Res. 53(Suppl 1): S69-S70.
    • (2004) Inflamm. Res. , vol.53 , pp. S69-S70
    • Cowart, M.1    Faghih, R.2    Gfesser, G.3
  • 121
    • 1642452635 scopus 로고    scopus 로고
    • A new class of potent non-imidazole H3 antagonists: 2-Aminoethylbenzofurans
    • Cowart, M., Pratt, J.K., Stewart, A.O. et al. 2004. A new class of potent non-imidazole H3 antagonists: 2-Aminoethylbenzofurans. Bioorg. Med. Chem. Lett. 14: 689-693.
    • (2004) Bioorg. Med. Chem. Lett. , vol.14 , pp. 689-693
    • Cowart, M.1    Pratt, J.K.2    Stewart, A.O.3
  • 122
    • 19944428635 scopus 로고    scopus 로고
    • 4-(2-[2-(2(R)-Methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention
    • Cowart, M., Faghih, R., Curtis, M.P. et al. 2005. 4-(2-[2-(2(R)-Methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. J. Med. Chem. 48: 38-55.
    • (2005) J. Med. Chem. , vol.48 , pp. 38-55
    • Cowart, M.1    Faghih, R.2    Curtis, M.P.3
  • 123
    • 85057687839 scopus 로고    scopus 로고
    • Pharmacological properties of novel, non-imidazole benzofuran H3 receptor antagonists
    • Washington, DC, April 17-21. Abst. #396.3
    • Miller, T.R., Krueger, K.M., Baranowski, J.L. et al. 2004. Pharmacological properties of novel, non-imidazole benzofuran H3 receptor antagonists. Experimental Biology, Washington, DC, April 17-21. Abst. #396.3.
    • (2004) Experimental Biology
    • Miller, T.R.1    Krueger, K.M.2    Baranowski, J.L.3
  • 124
    • 13844297634 scopus 로고    scopus 로고
    • A facile and scaleable synthesis of ABT-239, a benzofuranoid H3 antagonist
    • Pu, Y.M., Grieme, T., Gupta, A. et al. 2005. A facile and scaleable synthesis of ABT-239, a benzofuranoid H3 antagonist. Org. Proc. Res. Dev. 9: 45-50.
    • (2005) Org. Proc. Res. Dev. , vol.9 , pp. 45-50
    • Pu, Y.M.1    Grieme, T.2    Gupta, A.3
  • 125
    • 33748642181 scopus 로고    scopus 로고
    • An efficient and convergent synthesis of the potent and selective H3 antagonist ABT-239
    • Ku, Y.Y., Pu, Y.M., Grieme, T. et al. 2006. An efficient and convergent synthesis of the potent and selective H3 antagonist ABT-239. Tetrahedron 62: 4584-4589.
    • (2006) Tetrahedron , vol.62 , pp. 4584-4589
    • Ku, Y.Y.1    Pu, Y.M.2    Grieme, T.3
  • 126
    • 20144376337 scopus 로고    scopus 로고
    • Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties
    • Esbenshade, T.A., Fox, G.B., Krueger, K.M. et al. 2005. Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties. J. Pharmacol. Exp. Ther. 313: 165-175.
    • (2005) J. Pharmacol. Exp. Ther. , vol.313 , pp. 165-175
    • Esbenshade, T.A.1    Fox, G.B.2    Krueger, K.M.3
  • 127
    • 20144386364 scopus 로고    scopus 로고
    • Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist
    • Fox, G.B., Esbenshade, T.A., Pan, J.B. et al. 2005. Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist. J. Pharmacol. Exp. Ther. 313: 176-190.
    • (2005) J. Pharmacol. Exp. Ther. , vol.313 , pp. 176-190
    • Fox, G.B.1    Esbenshade, T.A.2    Pan, J.B.3
  • 128
    • 85057675941 scopus 로고    scopus 로고
    • ABT-239, a potent human histamine H3 receptor antagonist with favorable drug-like properties
    • San Diego, CA, March 31 to April 5. Abst. #321.7
    • Esbenshade, T.A., Wetter, J., Marsh, K. et al. 2005. ABT-239, a potent human histamine H3 receptor antagonist with favorable drug-like properties. Experimental Biol., San Diego, CA, March 31 to April 5. Abst. #321.7.
    • (2005) Experimental Biol.
    • Esbenshade, T.A.1    Wetter, J.2    Marsh, K.3
  • 129
    • 85057701634 scopus 로고    scopus 로고
    • Pharmacological properties of the S-enantiomer of the histamine H3 receptor antagonist ABT-239: An inverse agonist with no anti-obesity effects
    • San Diego, CA, March 31 to April 5. Abst. #85.9
    • Milicic, I., Krueger, K., Miller, T. et al. 2005. Pharmacological properties of the S-enantiomer of the histamine H3 receptor antagonist ABT-239: An inverse agonist with no anti-obesity effects. Experimental Biol., San Diego, CA, March 31 to April 5. Abst. #85.9.
    • (2005) Experimental Biol.
    • Milicic, I.1    Krueger, K.2    Miller, T.3
  • 130
    • 85057665496 scopus 로고    scopus 로고
    • ABT-239, a novel H3 receptor antagonist: Demonstration of a benign cardiovascular profile in the anesthetized canine
    • San Diego, CA, March 31 to April 5. Abst. #87.14
    • Preusser, L.C., Fryer, R.M., Esbenshade, T.A. et al. 2005. ABT-239, a novel H3 receptor antagonist: Demonstration of a benign cardiovascular profile in the anesthetized canine. Experimental Biol., San Diego, CA, March 31 to April 5. Abst. #87.14.
    • (2005) Experimental Biol.
    • Preusser, L.C.1    Fryer, R.M.2    Esbenshade, T.A.3
  • 132
    • 33947199306 scopus 로고    scopus 로고
    • Novel heterocyclic-substituted benzofuran histamine H3 receptor antagonists: In vitro properties, drug-likeness, and behavioral activity
    • Cowart, M., Gfesser, G.A., Browman, K.E. et al. 2007. Novel heterocyclic-substituted benzofuran histamine H3 receptor antagonists: In vitro properties, drug-likeness, and behavioral activity. Biochem. Pharmacol. 73: 1243-1255.
    • (2007) Biochem. Pharmacol. , vol.73 , pp. 1243-1255
    • Cowart, M.1    Gfesser, G.A.2    Browman, K.E.3
  • 133
    • 21144442005 scopus 로고    scopus 로고
    • Achievement of behavioral efficacy and improved potency in new heterocyclic analogs of benzofuran H3 antagonists
    • Cowart, M., Faghih, R., Gfesser, G. et al. 2005. Achievement of behavioral efficacy and improved potency in new heterocyclic analogs of benzofuran H3 antagonists. Inflamm. Res. 54: S25-S26.
    • (2005) Inflamm. Res. , vol.54 , pp. S25-S26
    • Cowart, M.1    Faghih, R.2    Gfesser, G.3
  • 134
    • 26444595613 scopus 로고    scopus 로고
    • Synthesis and SAR of 5-amino- and 5-(Aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency
    • Sun, M., Zhao, C., Gfesser, G.A. et al. 2005. Synthesis and SAR of 5-amino- and 5-(Aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency. J. Med. Chem. 48: 6482-6490.
    • (2005) J. Med. Chem. , vol.48 , pp. 6482-6490
    • Sun, M.1    Zhao, C.2    Gfesser, G.A.3
  • 135
    • 85057686128 scopus 로고    scopus 로고
    • Bicyclic heteroaromatic histamine H3 antagonists: Synthesis, potency, and in vivo profiles of analogs optimized for druglikeness
    • September 22, Cambridge, U.K
    • Cowart, M.D., Sun, M., Altenbach, R.A. et al. 2005. Bicyclic heteroaromatic histamine H3 antagonists: Synthesis, potency, and in vivo profiles of analogs optimized for druglikeness. XIII RSC-SCI Med. Chem. Symp. September 22, Cambridge, U.K.
    • (2005) XIII RSC-SCI Med. Chem. Symp.
    • Cowart, M.D.1    Sun, M.2    Altenbach, R.A.3
  • 139
    • 34447287933 scopus 로고    scopus 로고
    • Design, synthesis, and structureactivity relationship of novel non-imidazole histamine H3 antagonists
    • Washington, DC, August 28 to September 1. Abst. MEDI-103
    • Liu, H., Altenbach, R.J., Miller, T.R. et al. 2005. Design, synthesis, and structureactivity relationship of novel non-imidazole histamine H3 antagonists. 230th ACS National Meeting, Washington, DC, August 28 to September 1. Abst. MEDI-103.
    • (2005) 230th ACS National Meeting
    • Liu, H.1    Altenbach, R.J.2    Miller, T.R.3
  • 140
    • 33846997920 scopus 로고    scopus 로고
    • 4-[6-(2-Aminoethyl)naphthalen-2- yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration
    • Black, L.A., Nersesian, D.L., Sharma, P. et al. 2007. 4-[6-(2-Aminoethyl)naphthalen-2- yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration. Bioorg. Med. Chem. Lett. 17: 1443-1446.
    • (2007) Bioorg. Med. Chem. Lett. , vol.17 , pp. 1443-1446
    • Black, L.A.1    Nersesian, D.L.2    Sharma, P.3
  • 141
    • 85057662566 scopus 로고    scopus 로고
    • Optimization of H3 antagonist series for H3 selectivity over the hERG channel
    • Florence, Italy, May 9-13. Abst. O35
    • Cowart, M., Black, L., Liu, H. et al. 2007. Optimization of H3 antagonist series for H3 selectivity over the hERG channel. 36th European Histamine Research Soceity Meeting, Florence, Italy, May 9-13. Abst. O35.
    • (2007) 36th European Histamine Research Soceity Meeting
    • Cowart, M.1    Black, L.2    Liu, H.3
  • 142
    • 84858571292 scopus 로고    scopus 로고
    • Bicyclic heteroaromatic histamine H3 antagonists: Synthesis, potency, and in vivo profiles of analogs optimized for drug-likeness
    • Washington, DC, August 28 to September 1. Abst. MEDI-102
    • Altenbach, R.J., Liu, H., Esbenshade, T.A. et al. 2005. Bicyclic heteroaromatic histamine H3 antagonists: Synthesis, potency, and in vivo profiles of analogs optimized for drug-likeness. 230th ACS National Meeting, Washington, DC, August 28 to September 1. Abst. MEDI-102.
    • (2005) 230th ACS National Meeting
    • Altenbach, R.J.1    Liu, H.2    Esbenshade, T.A.3
  • 143
    • 85057659262 scopus 로고    scopus 로고
    • Effects of repeated H3 receptor antagonist administration on H3 receptor expression and function in rats
    • Milicic, I., Browman, K.E., Baranowski, J.L. et al. 2007. Effects of repeated H3 receptor antagonist administration on H3 receptor expression and function in rats. FASEB J. 21: A790-A79c.
    • (2007) FASEB J. , vol.21 , pp. A790-A879
    • Milicic, I.1    Browman, K.E.2    Baranowski, J.L.3
  • 144
    • 14044266671 scopus 로고    scopus 로고
    • Pre-clinical evaluation of novel H3 receptor antagonists
    • April 28 to May 2, Düsseldorf/Köln, Germany. Abst. O2
    • Medhurst, A.D. 2004. Pre-clinical evaluation of novel H3 receptor antagonists. 33th Eur. Histamine Res. Soc. Meeting, April 28 to May 2, Düsseldorf/Köln, Germany. Abst. O2.
    • (2004) 33th Eur. Histamine Res. Soc. Meeting
    • Medhurst, A.D.1
  • 145
    • 85057655171 scopus 로고    scopus 로고
    • GlaxoSmithkline website, 2007, http://www.gsk.com/investors/pp_pipeline_standard.htm.
    • (2007)
  • 147
    • 85057662105 scopus 로고    scopus 로고
    • Knowledge-based high throughput lead generation
    • Cambridge, U.K., September 22
    • Heightman, T.D. 2005. Knowledge-based high throughput lead generation. 13th RSCSCI Medicinal Chemistry Symposium, Cambridge, U.K., September 22.
    • (2005) 13th RSCSCI Medicinal Chemistry Symposium
    • Heightman, T.D.1
  • 148
    • 20444369889 scopus 로고    scopus 로고
    • Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists
    • Jin, J., Dhanak, D., Knight, S.D. et al. 2005. Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists. Bioorg. Med. Chem. Lett. 15: 3229-3232.
    • (2005) Bioorg. Med. Chem. Lett. , vol.15 , pp. 3229-3232
    • Jin, J.1    Dhanak, D.2    Knight, S.D.3
  • 149
    • 84858569658 scopus 로고    scopus 로고
    • The discovery of a novel series of potent, orally active histamine H3 receptor antagonists
    • Cambridge, U.K., September 22. delimi
    • Wilson, D.M. 2005. The discovery of a novel series of potent, orally active histamine H3 receptor antagonists. 13th RSC-SCI Medicinal Chemistry Symposium, Cambridge, U.K., September 22. delimi.
    • (2005) 13th RSC-SCI Medicinal Chemistry Symposium
    • Wilson, D.M.1
  • 152
    • 34248562939 scopus 로고    scopus 로고
    • GSK189254-a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer’s disease brain and improves cognitive performance in preclinical models
    • Medhurst, A.D., Atkins, A.R., Beresford, I.J. et al. 2007. GSK189254-a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer’s disease brain and improves cognitive performance in preclinical models. J. Pharmacol. Exp. Ther. 321: 1032-1045.
    • (2007) J. Pharmacol. Exp. Ther. , vol.321 , pp. 1032-1045
    • Medhurst, A.D.1    Atkins, A.R.2    Beresford, I.J.3
  • 153
    • 85057703551 scopus 로고    scopus 로고
    • The histamine H3 receptor antagonist GSK189254, improves performance in the rat novel object recognition and attentional set shifting tasks
    • 23-26 July, Oxford, U.K. Abst. TE12
    • Woolley, M., Gartlon, J., and Pemberton, D. 2006. The histamine H3 receptor antagonist GSK189254, improves performance in the rat novel object recognition and attentional set shifting tasks. BAP Summer Meeting, 23-26 July, Oxford, U.K. Abst. TE12.
    • (2006) BAP Summer Meeting
    • Woolley, M.1    Gartlon, J.2    Pemberton, D.3
  • 154
    • 85057670382 scopus 로고    scopus 로고
    • Detection of functional heterogeneity of histaminergic neurons in response to GSK189254, a novel H3 receptor antagonist
    • May 9-12, 2007, Florence, Italy. Abst. O6
    • Giannoni, P., Passani, M.B., Nosi, D. et al. 2007. Detection of functional heterogeneity of histaminergic neurons in response to GSK189254, a novel H3 receptor antagonist. 36th Eur. Histamine. Res. Soc. Meeting, May 9-12, 2007, Florence, Italy. Abst. O6.
    • (2007) 36th Eur. Histamine. Res. Soc. Meeting
    • Giannoni, P.1    Passani, M.B.2    Nosi, D.3
  • 155
    • 33947121092 scopus 로고    scopus 로고
    • Structurally novel histamine H3 receptor antagonists GSK207040 and GSK334429 improve scopolamine-induced memory impairment and capsaicin-induced secondary allodynia in rats
    • Medhurst, A.D., Briggs, M.A., Bruton, G. et al. 2007. Structurally novel histamine H3 receptor antagonists GSK207040 and GSK334429 improve scopolamine-induced memory impairment and capsaicin-induced secondary allodynia in rats. Biochem. Pharmacol. 73: 1182-1194.
    • (2007) Biochem. Pharmacol. , vol.73 , pp. 1182-1194
    • Medhurst, A.D.1    Briggs, M.A.2    Bruton, G.3
  • 160
    • 85057678175 scopus 로고    scopus 로고
    • Design and synthesis of novel histamine H3 antagonists: Potential therapeutics for the treament of alzheimers disease
    • Istanbul, Turkey. Abst. P288
    • Johnstone, V. 2006. Design and synthesis of novel histamine H3 antagonists: Potential therapeutics for the treament of alzheimers disease. The 19th International Symposium in Medicinal Chemistry (Part IV). Istanbul, Turkey. Abst. P288.
    • (2006) The 19th International Symposium in Medicinal Chemistry (Part IV).
    • Johnstone, V.1
  • 162
    • 34447291238 scopus 로고    scopus 로고
    • Novel potent H3 antagonists: Therapeutics for the treatment of dementia including alzheimer’s disease
    • Istanbul, Turkey. Abst. P247
    • Cooper, I.R., Abberley, L., and Briggs, M. 2006. Novel potent H3 antagonists: Therapeutics for the treatment of dementia including alzheimer’s disease. The 19th International Symposium in Medicinal Chemistry (Part IV). Istanbul, Turkey. Abst. P247.
    • (2006) The 19th International Symposium in Medicinal Chemistry (Part IV).
    • Cooper, I.R.1    Abberley, L.2    Briggs, M.3
  • 165
    • 2442637744 scopus 로고    scopus 로고
    • 1-Alkyl-4-acylpiperazines as a new class of imidazole-free histamine H3 receptor antagonists
    • Zaragoza, F., Stephensen, H., Knudsen, S.M. et al. 2004. 1-Alkyl-4-acylpiperazines as a new class of imidazole-free histamine H3 receptor antagonists. J. Med. Chem. 47: 2833-2838.
    • (2004) J. Med. Chem. , vol.47 , pp. 2833-2838
    • Zaragoza, F.1    Stephensen, H.2    Knudsen, S.M.3
  • 166
    • 2142694335 scopus 로고    scopus 로고
    • Cinnamic amides of (S)-2-(aminomethyl) pyrrolidines are potent H3 antagonists
    • Peschke, B., Bak, S., Hohlweg, R. et al. 2004. Cinnamic amides of (S)-2-(aminomethyl) pyrrolidines are potent H3 antagonists. Bioorg. Med. Chem. 12: 2603-2616.
    • (2004) Bioorg. Med. Chem. , vol.12 , pp. 2603-2616
    • Peschke, B.1    Bak, S.2    Hohlweg, R.3
  • 167
    • 33646183062 scopus 로고    scopus 로고
    • Benzo[b]thiophene-2-carboxamides and benzo[b]furan-2-carboxamides are potent antagonists of the human H3-receptor
    • Peschke, B., Bak, S., Hohlweg, R. et al. 2006. Benzo[b]thiophene-2-carboxamides and benzo[b]furan-2-carboxamides are potent antagonists of the human H3-receptor. Bioorg. Med. Chem. Lett. 16: 3162-3165.
    • (2006) Bioorg. Med. Chem. Lett. , vol.16 , pp. 3162-3165
    • Peschke, B.1    Bak, S.2    Hohlweg, R.3
  • 168
    • 33748306055 scopus 로고    scopus 로고
    • Ureas with histamine H3-antagonist receptor activity-A new scaffold discovered by lead-hopping from cinnamic acid amides
    • Lau, J.F., Jeppesen, C.B., Rimvall, K. et al. 2006. Ureas with histamine H3-antagonist receptor activity-A new scaffold discovered by lead-hopping from cinnamic acid amides. Bioorg. Med. Chem. Lett. 16: 5303-5308.
    • (2006) Bioorg. Med. Chem. Lett. , vol.16 , pp. 5303-5308
    • Lau, J.F.1    Jeppesen, C.B.2    Rimvall, K.3
  • 169
    • 12144273281 scopus 로고    scopus 로고
    • 2-(4-Alkyl-1-piperazinyl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists
    • Zaragoza, F., Stephensen, H., Peschke, B. et al. 2005. 2-(4-Alkyl-1-piperazinyl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists. J. Med. Chem. 48: 306-311.
    • (2005) J. Med. Chem. , vol.48 , pp. 306-311
    • Zaragoza, F.1    Stephensen, H.2    Peschke, B.3
  • 170
    • 33746649764 scopus 로고    scopus 로고
    • Synthesis and SAR of novel histamine H3 receptor antagonists
    • Jesudason, C.D., Beavers, L.S., Cramer, J.W. et al. 2006. Synthesis and SAR of novel histamine H3 receptor antagonists. Bioorg. Med. Chem. Lett. 16: 3415-3418.
    • (2006) Bioorg. Med. Chem. Lett. , vol.16 , pp. 3415-3418
    • Jesudason, C.D.1    Beavers, L.S.2    Cramer, J.W.3
  • 178
    • 85057690833 scopus 로고    scopus 로고
    • (3-Piperidin-1-ylpropoxy)- tetrahydroisoquinolines and tetra-hydroazepines: A novel series of selective histamine H3 receptor antagonists
    • Delphi, Greece, Abst
    • Jesudason, C.D., Beavers, L.S., and Cramer, J.W. 2006. (3-Piperidin-1-ylpropoxy)- tetrahydroisoquinolines and tetra-hydroazepines: A novel series of selective histamine H3 receptor antagonists. 35th Eur. Histamine Res. Soc. Meeting, Delphi, Greece, Abst. P11.
    • (2006) 35th Eur. Histamine Res. Soc. Meeting , pp. P11
    • Jesudason, C.D.1    Beavers, L.S.2    Cramer, J.W.3
  • 185
    • 85057701926 scopus 로고    scopus 로고
    • Histamine 3 receptor inverse agonists for the treatment of obesity. Biological and chemical challenges
    • Delphi, Greece, Abst. P8
    • Freichel, C., Arthur, S.G., and Hertel, C. 2006. Histamine 3 receptor inverse agonists for the treatment of obesity. Biological and chemical challenges. 35th Eur. Histamine Res. Soc. Meeting, Delphi, Greece, Abst. P8.
    • (2006) 35th Eur. Histamine Res. Soc. Meeting
    • Freichel, C.1    Arthur, S.G.2    Hertel, C.3
  • 190
    • 31344459084 scopus 로고    scopus 로고
    • Synthesis and biological evaluation of novel hexahydro-pyrido[3',2': 4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT2C receptor agonists
    • Richter, H.G.F., Adams, D.R., Benardeau, A. et al. 2006. Synthesis and biological evaluation of novel hexahydro-pyrido[3',2': 4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT2C receptor agonists. Bioorg. Med. Chem. Lett. 16: 1207-1211.
    • (2006) Bioorg. Med. Chem. Lett. , vol.16 , pp. 1207-1211
    • Richter, H.G.F.1    Adams, D.R.2    Benardeau, A.3
  • 193
    • 85057706446 scopus 로고    scopus 로고
    • US2006047114A1
    • Wlodecki, B. 2006. US2006047114A1.
    • (2006)
    • Wlodecki, B.1
  • 209
    • 85057700638 scopus 로고    scopus 로고
    • Benzimidazole-substituted (3-phenoxypropyl) amines as histamine H3 receptor ligands
    • San Francisco, CA, September 10-14, 2006. Abst. MEDI-501
    • Aslanian, R., Zhu, X., Tom, W. et al. 2006. Benzimidazole-substituted (3-phenoxypropyl) amines as histamine H3 receptor ligands. 232nd ACS National Meeting, San Francisco, CA, September 10-14, 2006. Abst. MEDI-501.
    • (2006) 232nd ACS National Meeting
    • Aslanian, R.1    Zhu, X.2    Tom, W.3
  • 216
    • 0035942507 scopus 로고    scopus 로고
    • Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE
    • De Esch, I.J.P., Mills, J.E.J., Perkins, T.D.J. et al. 2001. Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE. J. Med. Chem. 44: 1666-1674.
    • (2001) J. Med. Chem. , vol.44 , pp. 1666-1674
    • De Esch, I.J.P.1    Mills, J.E.J.2    Perkins, T.D.J.3
  • 217
    • 0033864709 scopus 로고    scopus 로고
    • A qualitative model for the histamine H3 receptor explaining agonistic and antagonistic activity simultaneously
    • Weinheim, Germany
    • De Esch, I.J.P., Timmerman, H., Menge, W.M.P.B. et al. 2000. A qualitative model for the histamine H3 receptor explaining agonistic and antagonistic activity simultaneously. Archiv der Pharmazie (Weinheim, Germany) 333: 254-260.
    • (2000) Archiv der Pharmazie , vol.333 , pp. 254-260
    • De Esch, I.J.P.1    Timmerman, H.2    Menge, W.M.P.B.3
  • 218
    • 0029348605 scopus 로고
    • Modelling and mutation studies on the histamine H1-receptor agonist binding site reveal different binding modes for H1-agonists: Asp116 (TM3) has a constitutive role in receptor stimulation
    • Ter Laak, A.M., Timmerman, H., Leurs, R. et al. 1995. Modelling and mutation studies on the histamine H1-receptor agonist binding site reveal different binding modes for H1-agonists: Asp116 (TM3) has a constitutive role in receptor stimulation. J. Comp.-Aided Mol. Design 9: 319-330.
    • (1995) J. Comp.-Aided Mol. Design , vol.9 , pp. 319-330
    • Ter Laak, A.M.1    Timmerman, H.2    Leurs, R.3
  • 219
    • 0034030530 scopus 로고    scopus 로고
    • Characterization of the binding site of the histamine H3 Receptor. 2. Synthesis, in vitro pharmacology, and QSAR of a series of monosubstituted benzyl analogues of thioperamide
    • Windhorst, A.D., Timmerman, H., Worthington, E.A. et al. 2000. Characterization of the binding site of the histamine H3 Receptor. 2. Synthesis, in vitro pharmacology, and QSAR of a series of monosubstituted benzyl analogues of thioperamide. J. Med. Chem. 43: 1754-1761.
    • (2000) J. Med. Chem. , vol.43 , pp. 1754-1761
    • Windhorst, A.D.1    Timmerman, H.2    Worthington, E.A.3
  • 220
    • 23944469920 scopus 로고    scopus 로고
    • Validation of a histamine H3 receptor model through structure-activity relationships for classical H3 antagonists
    • Lorenzi, S., Mor, M., Bordi, F. et al. 2005. Validation of a histamine H3 receptor model through structure-activity relationships for classical H3 antagonists. Bioorg. Med. Chem. 13: 5647-5657.
    • (2005) Bioorg. Med. Chem. , vol.13 , pp. 5647-5657
    • Lorenzi, S.1    Mor, M.2    Bordi, F.3
  • 221
    • 0036228908 scopus 로고    scopus 로고
    • The role of transmembrane helix 5 in agonist binding to the human H3 receptor
    • Uveges, A.J., Kowal, D., Zhang, Y. et al. 2002. The role of transmembrane helix 5 in agonist binding to the human H3 receptor. J. Pharmacol. Exp. Ther. 301: 451-458.
    • (2002) J. Pharmacol. Exp. Ther. , vol.301 , pp. 451-458
    • Uveges, A.J.1    Kowal, D.2    Zhang, Y.3
  • 222
    • 0028965667 scopus 로고
    • Pharmacological and functional characterisation of the wild-type and site-directed mutants of the human H1 histamine receptor stably expressed in CHO cells
    • Moguilevsky, N., Varsalona, F., Guillaume, J.P. et al. 1995. Pharmacological and functional characterisation of the wild-type and site-directed mutants of the human H1 histamine receptor stably expressed in CHO cells. J Recept. Signal Transduct. Res 15: 91-102.
    • (1995) J Recept. Signal Transduct. Res , vol.15 , pp. 91-102
    • Moguilevsky, N.1    Varsalona, F.2    Guillaume, J.P.3
  • 223
    • 0028227786 scopus 로고
    • Site-directed mutagenesis of the histamine H1-receptor reveals a selective interaction of asparagine207 with subclasses of H1-receptor agonists
    • Leurs, R., Smit, M.J., Tensen, C.P. et al. 1994. Site-directed mutagenesis of the histamine H1-receptor reveals a selective interaction of asparagine207 with subclasses of H1-receptor agonists. Biochem. Biophys. Res. Commun. 201: 295-301.
    • (1994) Biochem. Biophys. Res. Commun. , vol.201 , pp. 295-301
    • Leurs, R.1    Smit, M.J.2    Tensen, C.P.3
  • 224
    • 0026644846 scopus 로고
    • Molecular basis for the interaction of histamine with the histamine H2 receptor
    • Gantz, I., DelValle, J., Wang, L.D. et al. 1992. Molecular basis for the interaction of histamine with the histamine H2 receptor. J. Biol. Chem. 267: 20840-20843.
    • (1992) J. Biol. Chem. , vol.267 , pp. 20840-20843
    • Gantz, I.1    DelValle, J.2    Wang, L.D.3
  • 225
    • 0036089526 scopus 로고    scopus 로고
    • Molecular modeling and site-specific mutagenesis of the histamine-binding site of the histamine H4 receptor
    • Shin, N., Coates, E., Murgolo, N.J. et al. 2002. Molecular modeling and site-specific mutagenesis of the histamine-binding site of the histamine H4 receptor. Mol. Pharmacol. 62: 38-47.
    • (2002) Mol. Pharmacol. , vol.62 , pp. 38-47
    • Shin, N.1    Coates, E.2    Murgolo, N.J.3
  • 226
    • 0034787251 scopus 로고    scopus 로고
    • Three-dimensional representations of G protein-coupled receptor structures and mechanisms
    • Visiers, I., Ballesteros, J.A., and Weinstein, H. 2002. Three-dimensional representations of G protein-coupled receptor structures and mechanisms. Methods Enzymol. 343: 329-371.
    • (2002) Methods Enzymol. , vol.343 , pp. 329-371
    • Visiers, I.1    Ballesteros, J.A.2    Weinstein, H.3
  • 227
    • 33746894730 scopus 로고    scopus 로고
    • Dibasic non-imidazole histamine H3 receptor antagonists with a rigid biphenyl scaffold
    • Morini, G., Comini, M., Rivara, M. et al. 2006. Dibasic non-imidazole histamine H3 receptor antagonists with a rigid biphenyl scaffold. Bioorg. Med. Chem. Lett. 16: 4063-4067.
    • (2006) Bioorg. Med. Chem. Lett. , vol.16 , pp. 4063-4067
    • Morini, G.1    Comini, M.2    Rivara, M.3
  • 228
    • 0035832108 scopus 로고    scopus 로고
    • Different antagonist binding properties of human and rat histamine H3 receptors
    • Stark, H., Sippl, W., Ligneau, X. et al. 2001. Different antagonist binding properties of human and rat histamine H3 receptors. Bioorg. Med. Chem. Lett. 11: 951-954.
    • (2001) Bioorg. Med. Chem. Lett. , vol.11 , pp. 951-954
    • Stark, H.1    Sippl, W.2    Ligneau, X.3
  • 229
    • 0033638021 scopus 로고    scopus 로고
    • Distinct pharmacology of rat and human histamine H3 receptors: Role of two amino acids in the third transmembrane domain
    • Ligneau, X., Morisset, S., Tardivel-Lacombe, J. et al. 2000. Distinct pharmacology of rat and human histamine H3 receptors: Role of two amino acids in the third transmembrane domain. Br. J. Pharmacol. 131: 1247-1250.
    • (2000) Br. J. Pharmacol. , vol.131 , pp. 1247-1250
    • Ligneau, X.1    Morisset, S.2    Tardivel-Lacombe, J.3
  • 230
    • 0037401965 scopus 로고    scopus 로고
    • Molecular modeling and pharmacological analysis of species-related histamine H3 receptor heterogeneity
    • Yao, B.B., Hutchins, C.W., Carr, T.L. et al. 2003. Molecular modeling and pharmacological analysis of species-related histamine H3 receptor heterogeneity. Neuropharmacol. 44: 773-786.
    • (2003) Neuropharmacol. , vol.44 , pp. 773-786
    • Yao, B.B.1    Hutchins, C.W.2    Carr, T.L.3
  • 231
    • 13444267334 scopus 로고    scopus 로고
    • Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes
    • Boeckler, F., Lanig, H., and Gmeiner, P. 2005. Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes. J. Med. Chem. 48: 694-709.
    • (2005) J. Med. Chem. , vol.48 , pp. 694-709
    • Boeckler, F.1    Lanig, H.2    Gmeiner, P.3
  • 232
    • 0033118334 scopus 로고    scopus 로고
    • Molecular tinkering of G protein-coupled receptors: An evolutionary success
    • Bockaert, J. and Pin, J.P. 1999. Molecular tinkering of G protein-coupled receptors: An evolutionary success. EMBO J. 18: 1723-1729.
    • (1999) EMBO J. , vol.18 , pp. 1723-1729
    • Bockaert, J.1    Pin, J.P.2
  • 233
    • 0027374544 scopus 로고
    • Protonation states of membrane- embedded carboxylic acid groups in rhodopsin and metarhodopsin II: A Fourier-transform infrared spectroscopy study of site-directed mutants
    • Fahmy, K., Jager, F., Beck, M. et al. 1993. Protonation states of membrane- embedded carboxylic acid groups in rhodopsin and metarhodopsin II: A Fourier-transform infrared spectroscopy study of site-directed mutants. Proc. Natl Acad. Sci. U.S.A. 90: 10206-10210.
    • (1993) Proc. Natl Acad. Sci. U.S.A. , vol.90 , pp. 10206-10210
    • Fahmy, K.1    Jager, F.2    Beck, M.3
  • 234
    • 0037197848 scopus 로고    scopus 로고
    • Functional role of internal water molecules in rhodopsin revealed by X-ray crystallography
    • Okada, T., Fujiyoshi, Y., Silow, M. et al. 2002. Functional role of internal water molecules in rhodopsin revealed by X-ray crystallography. Proc. Natl Acad. Sci. U.S.A. 99: 5982-5987.
    • (2002) Proc. Natl Acad. Sci. U.S.A. , vol.99 , pp. 5982-5987
    • Okada, T.1    Fujiyoshi, Y.2    Silow, M.3
  • 235
    • 33646004318 scopus 로고    scopus 로고
    • Three-dimensional models of histamine H3 receptor antagonist complexes and their pharmacophore
    • Axe, F.U., Bembenek, S.D., and Szalma, S. 2006. Three-dimensional models of histamine H3 receptor antagonist complexes and their pharmacophore. J. Mol. Graph. Model. 24: 456-464.
    • (2006) J. Mol. Graph. Model. , vol.24 , pp. 456-464
    • Axe, F.U.1    Bembenek, S.D.2    Szalma, S.3
  • 237
    • 21144432460 scopus 로고    scopus 로고
    • Model of a specific human histamine H3 receptor (hH3R) binding pocket suitable for virtual drug design
    • Schlegel, B., Stark, H., Sippl, W. et al. 2005. Model of a specific human histamine H3 receptor (hH3R) binding pocket suitable for virtual drug design. Inflamm. Res. 54: S50-S51.
    • (2005) Inflamm. Res. , vol.54 , pp. S50-S51
    • Schlegel, B.1    Stark, H.2    Sippl, W.3
  • 238
    • 34250892426 scopus 로고    scopus 로고
    • Pharmacophore refinement and 3D-QSAR studies of histamine H3 antagonists
    • Narkhede, S.S. and Degani, M.S. 2007. Pharmacophore refinement and 3D-QSAR studies of histamine H3 antagonists. QSAR Combi. Sci. 26: 744-753.
    • (2007) QSAR Combi. Sci. , vol.26 , pp. 744-753
    • Narkhede, S.S.1    Degani, M.S.2
  • 239
    • 77957057769 scopus 로고    scopus 로고
    • Synthesis of radioligands for the histamine H3 receptor
    • Eds R. Leurs, H. Timmerman, Elsevier, Amsterdam
    • Jansen, F.P., Leurs, R., and Timmerman, H. 1998. Synthesis of radioligands for the histamine H3 receptor. In: The Histamine H3 Receptor: A Target for New Drugs. Eds R. Leurs, H. Timmerman, Elsevier, Amsterdam: pp. 127-144.
    • (1998) The Histamine H3 Receptor: A Target for New Drugs , pp. 127-144
    • Jansen, F.P.1    Leurs, R.2    Timmerman, H.3
  • 240
    • 85057657360 scopus 로고    scopus 로고
    • Synthesis of radioligands for the histamine H3 receptor
    • Eds R. Leurs, H. Timmerman, Elsevier, Amsterdam
    • Windhorst, A.D., Leurs, R., Menge, W.M. et al. 1998. Synthesis of radioligands for the histamine H3 receptor. In: The Histamine H3 Receptor: A Target for New Drugs. Eds R. Leurs, H. Timmerman, Elsevier, Amsterdam: pp. 139-174.
    • (1998) The Histamine H3 Receptor: A Target for New Drugs , pp. 139-174
    • Windhorst, A.D.1    Leurs, R.2    Menge, W.M.3
  • 241
    • 21144439214 scopus 로고    scopus 로고
    • Use of novel, non-imidazole inverse agonist radioligands to define histamine H3 receptor pharmacology
    • Esbenshade, T.A., Yao, B.B., Witte, D.G. et al. 2005. Use of novel, non-imidazole inverse agonist radioligands to define histamine H3 receptor pharmacology. Inflamm. Res. 54: S46-S47.
    • (2005) Inflamm. Res. , vol.54 , pp. S46-S47
    • Esbenshade, T.A.1    Yao, B.B.2    Witte, D.G.3
  • 242
    • 32144443291 scopus 로고    scopus 로고
    • Use of an inverse agonist radioligand [3H]A-317920 reveals distinct pharmacological profiles of the rat histamine H3 receptor
    • Yao, B.B., Witte, D.G., Miller, T.R. et al. 2006. Use of an inverse agonist radioligand [3H]A-317920 reveals distinct pharmacological profiles of the rat histamine H3 receptor. Neuropharmacology 50: 468-478.
    • (2006) Neuropharmacology , vol.50 , pp. 468-478
    • Yao, B.B.1    Witte, D.G.2    Miller, T.R.3
  • 243
    • 33745621937 scopus 로고    scopus 로고
    • Detection of multiple H3 receptor affinity states utilizing [3H]A-349821, a novel, selective, non-imidazole histamine H3 receptor inverse agonist radioligand
    • Witte, D.G., Yao, B.B., Miller, T.R. et al. 2006. Detection of multiple H3 receptor affinity states utilizing [3H]A-349821, a novel, selective, non-imidazole histamine H3 receptor inverse agonist radioligand. Br. J. Pharmacol. 148: 657-670.
    • (2006) Br. J. Pharmacol. , vol.148 , pp. 657-670
    • Witte, D.G.1    Yao, B.B.2    Miller, T.R.3
  • 244
    • 8744233669 scopus 로고    scopus 로고
    • Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist
    • Barbier, A.J., Berridge, C., Dugovic, C. et al. 2004. Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br. J. Pharmacol. 143: 649-661.
    • (2004) Br. J. Pharmacol. , vol.143 , pp. 649-661
    • Barbier, A.J.1    Berridge, C.2    Dugovic, C.3
  • 245
    • 33747352284 scopus 로고    scopus 로고
    • Radiosynthesis and biodistribution of a histamine H3 receptor antagonist 4-[3-(4-piperidin-1-yl-but-1-ynyl)-[11C]benzyl]-morpholine: Evaluation of a potential PET ligand
    • Airaksinen, A.J., Jablonowski, J.A., van der, M.M. et al. 2006. Radiosynthesis and biodistribution of a histamine H3 receptor antagonist 4-[3-(4-piperidin-1-yl-but-1-ynyl)-[11C]benzyl]-morpholine: Evaluation of a potential PET ligand. Nucl. Med. Biol. 33: 801-810.
    • (2006) Nucl. Med. Biol. , vol.33 , pp. 801-810
    • Airaksinen, A.J.1    Jablonowski, J.A.2    van der, M.M.3
  • 246
    • 85057674067 scopus 로고    scopus 로고
    • WO2006072596A1
    • Plisson, C. 2006. WO2006072596A1.
    • (2006)
    • Plisson, C.1
  • 247
    • 33646773584 scopus 로고    scopus 로고
    • Fluorescent benzofuran histamine H3 receptor antagonists with sub-nanomolar potency
    • Cowart, M., Gfesser, G.A., Bhatia, K. et al. 2006. Fluorescent benzofuran histamine H3 receptor antagonists with sub-nanomolar potency. Inflamm. Res. 55: S47-S48.
    • (2006) Inflamm. Res. , vol.55 , pp. S47-S48
    • Cowart, M.1    Gfesser, G.A.2    Bhatia, K.3
  • 248
    • 35148873534 scopus 로고    scopus 로고
    • Highly potent fluorescence-tagged nonimidazole histamine H3 receptor ligands
    • Amon, M., Ligneau, X., Camelin, J.C. et al. 2007. Highly potent fluorescence-tagged nonimidazole histamine H3 receptor ligands. Chem. Med. Chem. 2: 708-716.
    • (2007) Chem. Med. Chem. , vol.2 , pp. 708-716
    • Amon, M.1    Ligneau, X.2    Camelin, J.C.3
  • 250
    • 33845762340 scopus 로고    scopus 로고
    • Multi-target therapeutics: When the whole is greater than the sum of the parts
    • Zimmermann, G.R., Lehar, J., and Keith, C.T. 2007. Multi-target therapeutics: When the whole is greater than the sum of the parts. Drug Disc. Today 12: 34-42.
    • (2007) Drug Disc. Today , vol.12 , pp. 34-42
    • Zimmermann, G.R.1    Lehar, J.2    Keith, C.T.3
  • 251
    • 26944497552 scopus 로고    scopus 로고
    • Nasal allergic response mediated by histamine H3 receptors in murine allergic rhinitis
    • Nakaya, M., Fukushima, Y., Takeuchi, N. et al. 2005. Nasal allergic response mediated by histamine H3 receptors in murine allergic rhinitis. Laryngoscope 115: 1778-1784.
    • (2005) Laryngoscope , vol.115 , pp. 1778-1784
    • Nakaya, M.1    Fukushima, Y.2    Takeuchi, N.3
  • 252
    • 13444301282 scopus 로고    scopus 로고
    • Effect of combined histamine H1 and H3 receptor blockade on cutaneous microvascular permeability elicited by compound 48/80
    • McLeod, R.L., Mingo, G.G., Kreutner, W. et al. 2005. Effect of combined histamine H1 and H3 receptor blockade on cutaneous microvascular permeability elicited by compound 48/80. Life Sci. 76: 1787-1794.
    • (2005) Life Sci. , vol.76 , pp. 1787-1794
    • McLeod, R.L.1    Mingo, G.G.2    Kreutner, W.3
  • 253
    • 0038814244 scopus 로고    scopus 로고
    • Pharmacological characterization of the novel histamine H3-receptor antagonist N-(3,5-dichlorophenyl)-N’-[[4-(1H-imidazol-4-ylmethyl)phenyl]methyl]urea (SCH 79687)
    • McLeod, R.L., Rizzo, C.A., West, R.E., Jr. et al. 2003. Pharmacological characterization of the novel histamine H3-receptor antagonist N-(3,5-dichlorophenyl)-N’-[[4-(1H-imidazol-4-ylmethyl)phenyl]methyl]urea (SCH 79687). J. Pharmacol. Exp. Ther. 305: 1037-1044.
    • (2003) J. Pharmacol. Exp. Ther. , vol.305 , pp. 1037-1044
    • McLeod, R.L.1    Rizzo, C.A.2    West, R.E.3
  • 254
    • 18744369679 scopus 로고    scopus 로고
    • Histamine-mediated mechanisms in the human nasal airway
    • Taylor-Clark, T. and Foreman, J. 2005. Histamine-mediated mechanisms in the human nasal airway. Curr. Opin. Pharmacol. 5: 214-220.
    • (2005) Curr. Opin. Pharmacol. , vol.5 , pp. 214-220
    • Taylor-Clark, T.1    Foreman, J.2
  • 255
    • 33144473095 scopus 로고    scopus 로고
    • H1 antihistamines: Patent highlights 2000-2005
    • Fonquerna, S. and Miralpeix, M. 2006. H1 antihistamines: Patent highlights 2000-2005. Expert Opin. Ther. Pat. 16: 109-117.
    • (2006) Expert Opin. Ther. Pat. , vol.16 , pp. 109-117
    • Fonquerna, S.1    Miralpeix, M.2
  • 259
    • 3242794178 scopus 로고    scopus 로고
    • From magic bullets to designed multiple ligands
    • Morphy, R., Kay, C., and Rankovic, Z. 2004. From magic bullets to designed multiple ligands. Drug Disc. Today 9: 641-651.
    • (2004) Drug Disc. Today , vol.9 , pp. 641-651
    • Morphy, R.1    Kay, C.2    Rankovic, Z.3
  • 260
    • 0030594996 scopus 로고    scopus 로고
    • Diphenylmethyl ethers: Synthesis and histamine H3-receptor antagonist in vitro and in vivo activity
    • Huls, A., Purand, K., Stark, H. et al. 1996. Diphenylmethyl ethers: Synthesis and histamine H3-receptor antagonist in vitro and in vivo activity. Bioorg. Med. Chem. Lett. 6: 2013-2018.
    • (1996) Bioorg. Med. Chem. Lett. , vol.6 , pp. 2013-2018
    • Huls, A.1    Purand, K.2    Stark, H.3
  • 261
    • 18344368989 scopus 로고    scopus 로고
    • Identification of a novel, orally bioavailable histamine H3 receptor antagonist based on the 4-benzyl-(1H-imidazol-4-yl) template
    • Aslanian, R., Mutahi, M.W., Shih, N.Y. et al. 2002. Identification of a novel, orally bioavailable histamine H3 receptor antagonist based on the 4-benzyl-(1H-imidazol-4-yl) template. Bioorg. Med. Chem. Lett. 12: 937-941.
    • (2002) Bioorg. Med. Chem. Lett. , vol.12 , pp. 937-941
    • Aslanian, R.1    Mutahi, M.W.2    Shih, N.Y.3
  • 263
    • 85057674931 scopus 로고    scopus 로고
    • Novel potent dual histamine H1/H3 receptor antagonists
    • May 9-12 2007, Florence, Italy. Abst. P33
    • Isensee, K., Amon, M., and Sasse, B. 2007. Novel potent dual histamine H1/H3 receptor antagonists. 36th European Histamine Research Society Meeting, May 9-12 2007, Florence, Italy. Abst. P33.
    • (2007) 36th European Histamine Research Society Meeting
    • Isensee, K.1    Amon, M.2    Sasse, B.3
  • 264
    • 2142737534 scopus 로고    scopus 로고
    • A new class of NO-donor H3-antagonists
    • Tosco, P., Bertinaria, M., Di Stilo, A. et al. 2004. A new class of NO-donor H3-antagonists. Farmaco 59: 359-371.
    • (2004) Farmaco , vol.59 , pp. 359-371
    • Tosco, P.1    Bertinaria, M.2    Di Stilo, A.3
  • 265
    • 21744461467 scopus 로고    scopus 로고
    • Non-imidazole histamine NO-donor H3-antagonists
    • Tosco, P., Bertinaria, M., Di Stilo, A. et al. 2005. Non-imidazole histamine NO-donor H3-antagonists. Farmaco 60: 507-512.
    • (2005) Farmaco , vol.60 , pp. 507-512
    • Tosco, P.1    Bertinaria, M.2    Di Stilo, A.3
  • 266
    • 20544434620 scopus 로고    scopus 로고
    • Furoxan analogues of the histamine H3-receptor antagonist imoproxifan and related furazan derivatives
    • Tosco, P., Bertinaria, M., Di Stilo, A. et al. 2005. Furoxan analogues of the histamine H3-receptor antagonist imoproxifan and related furazan derivatives. Bioorg. Med. Chem. 13: 4750-4759.
    • (2005) Bioorg. Med. Chem. , vol.13 , pp. 4750-4759
    • Tosco, P.1    Bertinaria, M.2    Di Stilo, A.3
  • 267
    • 33947683747 scopus 로고    scopus 로고
    • Recent advances in the development of hybrid molecules/designed multiple compounds with antiamnesic properties
    • Decker, M. 2007. Recent advances in the development of hybrid molecules/designed multiple compounds with antiamnesic properties. Mini-Rev. Med. Chem. 7: 221-229.
    • (2007) Mini-Rev. Med. Chem. , vol.7 , pp. 221-229
    • Decker, M.1
  • 268
    • 33644851841 scopus 로고    scopus 로고
    • Dimeric and hybrid anti-alzheimer drug candidates
    • Muñoz-Torrero, D. and Camps, P. 2006. Dimeric and hybrid anti-alzheimer drug candidates. Curr. Med. Chem. 13: 399-422.
    • (2006) Curr. Med. Chem. , vol.13 , pp. 399-422
    • Muñoz-Torrero, D.1    Camps, P.2
  • 269
    • 0037186501 scopus 로고    scopus 로고
    • Development of a new class of nonimidazole histamine H3 receptor ligands with combined inhibitory histamine N-methyltransferase activity
    • Apelt, J., Ligneau, X., Pertz, H.H. et al. 2002. Development of a new class of nonimidazole histamine H3 receptor ligands with combined inhibitory histamine N-methyltransferase activity. J. Med. Chem. 45: 1128-1141.
    • (2002) J. Med. Chem. , vol.45 , pp. 1128-1141
    • Apelt, J.1    Ligneau, X.2    Pertz, H.H.3
  • 270
    • 14244268026 scopus 로고    scopus 로고
    • Search for histamine H3 receptor antagonists with combined inhibitory potency at Nt-methyltransferase: Ether derivatives
    • Apelt, J., Grassmann, S., Ligneau, X. et al. 2005. Search for histamine H3 receptor antagonists with combined inhibitory potency at Nt-methyltransferase: Ether derivatives. Pharmazie 60: 97-106.
    • (2005) Pharmazie , vol.60 , pp. 97-106
    • Apelt, J.1    Grassmann, S.2    Ligneau, X.3
  • 271
    • 0037447913 scopus 로고    scopus 로고
    • Imidazole derivatives as a novel class of hybrid compounds with inhibitory histamine N-methyltransferase potencies and histamine H3 receptor affinities
    • Grassmann, S., Apelt, J., Sippl, W. et al. 2003. Imidazole derivatives as a novel class of hybrid compounds with inhibitory histamine N-methyltransferase potencies and histamine H3 receptor affinities. Bioorg. Med. Chem. 11: 2163-2174.
    • (2003) Bioorg. Med. Chem. , vol.11 , pp. 2163-2174
    • Grassmann, S.1    Apelt, J.2    Sippl, W.3
  • 272
    • 8444225402 scopus 로고    scopus 로고
    • Search for histamine H(3) receptor ligands with combined inhibitory potency at histamine N-methyltransferase: Omegapiperidinoalkanamine derivatives
    • Grassmann, S., Apelt, J., Ligneau, X. et al. 2004. Search for histamine H(3) receptor ligands with combined inhibitory potency at histamine N-methyltransferase: Omegapiperidinoalkanamine derivatives. Arch. Pharm. (Weinheim) 337: 533-545.
    • (2004) Arch. Pharm. (Weinheim) , vol.337 , pp. 533-545
    • Grassmann, S.1    Apelt, J.2    Ligneau, X.3
  • 273
    • 33645361406 scopus 로고    scopus 로고
    • Multiple enzyme inhibitions by histamine H3 receptor antagonists as potential procognitive agents
    • Petroianu, G., Arafat, K., Sasse, B.C. et al. 2006. Multiple enzyme inhibitions by histamine H3 receptor antagonists as potential procognitive agents. Pharmazie 61: 179-182.
    • (2006) Pharmazie , vol.61 , pp. 179-182
    • Petroianu, G.1    Arafat, K.2    Sasse, B.C.3
  • 274
    • 25144443484 scopus 로고    scopus 로고
    • Structural basis for inhibition of histamine N-methyltransferase by diverse drugs
    • Horton, J.R., Sawada, K., Nishibori, M. et al. 2005. Structural basis for inhibition of histamine N-methyltransferase by diverse drugs. J. Mol. Biol. 353: 334-344.
    • (2005) J. Mol. Biol. , vol.353 , pp. 334-344
    • Horton, J.R.1    Sawada, K.2    Nishibori, M.3
  • 275
    • 33646834939 scopus 로고    scopus 로고
    • Modulation of spontaneous alternation performance of mice treated with thioperamide and tacrine in a cross maze task
    • Vohora, D., Pal, S.N., and Pillai, K.K. 2005. Modulation of spontaneous alternation performance of mice treated with thioperamide and tacrine in a cross maze task. Fundam. Clin. Pharmacol. 19: 531-532.
    • (2005) Fundam. Clin. Pharmacol. , vol.19 , pp. 531-532
    • Vohora, D.1    Pal, S.N.2    Pillai, K.K.3
  • 277
    • 33846173583 scopus 로고    scopus 로고
    • Developing selectively nonselective drugs for treating CNS disorders
    • Gray, J.A. and Roth, B.L. 2006. Developing selectively nonselective drugs for treating CNS disorders. Drug Discov. Today Ther. Strat. 3: 413-419.
    • (2006) Drug Discov. Today Ther. Strat. , vol.3 , pp. 413-419
    • Gray, J.A.1    Roth, B.L.2
  • 278
    • 33846186881 scopus 로고    scopus 로고
    • Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore
    • Keith, J.M., Gomez, L.A., Letavic, M.A. et al. 2007. Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore. Bioorg. Med. Chem. Lett. 17: 702-706.
    • (2007) Bioorg. Med. Chem. Lett. , vol.17 , pp. 702-706
    • Keith, J.M.1    Gomez, L.A.2    Letavic, M.A.3
  • 279
    • 33846618166 scopus 로고    scopus 로고
    • Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors
    • Letavic, M.A., Keith, J.M., Jablonowski, J.A. et al. 2007. Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors. Bioorg. Med. Chem. Lett. 17: 1047-1051.
    • (2007) Bioorg. Med. Chem. Lett. , vol.17 , pp. 1047-1051
    • Letavic, M.A.1    Keith, J.M.2    Jablonowski, J.A.3
  • 280
    • 33947715270 scopus 로고    scopus 로고
    • Pyrrolidino-tetrahydroisoquinolines as potent dual H3 antagonist and serotonin transporter inhibitors
    • Keith, J.M., Gomez, L.A., Wolin, R.L. et al. 2007. Pyrrolidino-tetrahydroisoquinolines as potent dual H3 antagonist and serotonin transporter inhibitors. Bioorg. Med. Chem. Lett. 17: 2603-2607.
    • (2007) Bioorg. Med. Chem. Lett. , vol.17 , pp. 2603-2607
    • Keith, J.M.1    Gomez, L.A.2    Wolin, R.L.3
  • 281
    • 33947731437 scopus 로고    scopus 로고
    • Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors
    • Letavic, M.A., Keith, J.M., Ly, K.S. et al. 2007. Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors. Bioorg. Med. Chem. Lett. 17: 2566-2569.
    • (2007) Bioorg. Med. Chem. Lett. , vol.17 , pp. 2566-2569
    • Letavic, M.A.1    Keith, J.M.2    Ly, K.S.3
  • 282
    • 40849137722 scopus 로고    scopus 로고
    • 3 receptor improves wakefulness in narcolepsy: Studies in orexin-/- mice and patients
    • 3 receptor improves wakefulness in narcolepsy: studies in orexin-/- mice and patients. Neurobiol. Dis. 30(1): 74-83.
    • (2008) Neurobiol. Dis , vol.30 , Issue.1 , pp. 74-83
    • Lin, J.S.1    Dauvilliers, Y.2    Arnulf, I.3
  • 283
    • 85057669789 scopus 로고    scopus 로고
    • JP Morgan 24th Annual Healthcare Conference, San Francisco, CA, January, Cephalon website
    • JP Morgan 24th Annual Healthcare Conference, San Francisco, CA, January 2006, Cephalon website, www.cephalon.com.
    • (2006)
  • 284
    • 85057677498 scopus 로고    scopus 로고
    • February, Cephalon website
    • Merrill Lynch Global Pharmaceutical, Biotechnology and Medical Device Conference, February 2007, Cephalon website, www.cephalon.com.
    • (2007)
  • 285
    • 85057683960 scopus 로고    scopus 로고
    • Neurology, GlaxoSmithKline website
    • Hunter, J. Neurology, GlaxoSmithKline website, http://www.gsk.com/investors/presen tations_webcasts04.htm.
    • Hunter, J.1
  • 286
    • 85057690891 scopus 로고    scopus 로고
    • Psychiatry, GlaxoSmithKline website
    • Ratti, E. Psychiatry, GlaxoSmithKline website, http://www.gsk.com/investors/presen tations_webcasts04.htm.
    • Ratti, E.1
  • 287
    • 85057664848 scopus 로고    scopus 로고
    • http://www.schizophreniaforum.org/res/trials/all.pdf.
  • 288
    • 85057656644 scopus 로고    scopus 로고
    • Effectiveness of the drug GSK189254 in treating patients with narcolepsy
    • Effectiveness of the drug GSK189254 in treating patients with narcolepsy, http://clinicaltrials.gov/show/NCT00366080.
  • 292
    • 34147140063 scopus 로고    scopus 로고
    • A H3 antagonist for treating allergic rhinitis: A development candidate?
    • Norman, P. 2007. A H3 antagonist for treating allergic rhinitis: A development candidate? Expert Opin. Ther. Pat. 17: 449-452.
    • (2007) Expert Opin. Ther. Pat. , vol.17 , pp. 449-452
    • Norman, P.1
  • 293
    • 0032590015 scopus 로고    scopus 로고
    • Combined histamine H1 and H3 receptor blockade produces nasal decongestion in an experimental model of nasal congestion
    • McLeod, R.L., Mingo, G.G., Herczku, C. et al. 1999. Combined histamine H1 and H3 receptor blockade produces nasal decongestion in an experimental model of nasal congestion. Am. J. Rhinol. 13: 391-399.
    • (1999) Am. J. Rhinol. , vol.13 , pp. 391-399
    • McLeod, R.L.1    Mingo, G.G.2    Herczku, C.3
  • 294
    • 85057657477 scopus 로고    scopus 로고
    • http://www.stanleyresearch.org/Trial/Drug/AwardedTrial.aspx.
  • 295
    • 85057654803 scopus 로고    scopus 로고
    • http://www.schizophreniaforum.org/res/trials/all.pdf.
  • 297
    • 85057693176 scopus 로고    scopus 로고
    • WO2006084833A1
    • Raga, M.M. et al. 2006. WO2006084833A1.
    • (2006)
    • Raga, M.M.1
  • 299
    • 85057668172 scopus 로고    scopus 로고
    • Sanofi-Aventis website, http://www.sanofi-aventis.com/rd/portfolio/p_rd_portfolio_ snc.asp.
  • 300
    • 36749011925 scopus 로고    scopus 로고
    • Molecular modeling of histamine H3 receptor and QSAR studies on arylbenzofuran derived H3 antagonists
    • Dastmalchi, S., Hamzeh-Mivehroud, M., Ghafourian, T. et al. 2007. Molecular modeling of histamine H3 receptor and QSAR studies on arylbenzofuran derived H3 antagonists. J. Mol. Graph. Model. 26(5): 834-844.
    • (2007) J. Mol. Graph. Model. , vol.26 , Issue.5 , pp. 834-844
    • Dastmalchi, S.1    Hamzeh-Mivehroud, M.2    Ghafourian, T.3
  • 301
    • 34250179519 scopus 로고    scopus 로고
    • A new class of histamine H3 receptor antagonists derived from ligand based design
    • Roche, O. and Rodriguez Sarmiento, R.M. 2007. A new class of histamine H3 receptor antagonists derived from ligand based design. Bioorg. Med. Chem. Lett. 17: 3670-3675.
    • (2007) Bioorg. Med. Chem. Lett. , vol.17 , pp. 3670-3675
    • Roche, O.1    Rodriguez Sarmiento, R.M.2
  • 302
    • 85057709747 scopus 로고    scopus 로고
    • Identification of histamine H3 receptor antagonists
    • Del Tredici, A.L., Eskildsen, J., Andersen, C.B. et al. 2007. Identification of histamine H3 receptor antagonists. FASEB J. 21: A790-A79d.
    • (2007) FASEB J. , vol.21 , pp. A790-A879
    • Del Tredici, A.L.1    Eskildsen, J.2    Andersen, C.B.3
  • 303
    • 85057684209 scopus 로고    scopus 로고
    • Fixed-combination therapies for the treatment of CNS disorders. Analysis of current trends and future prospects among U.S. physicians and HMOs
    • November, 2004
    • DiModica, L. 2004. Fixed-combination therapies for the treatment of CNS disorders. Analysis of current trends and future prospects among U.S. physicians and HMOs. Decision Resour. November 2004.
    • (2004) Decision Resour.
    • DiModica, L.1
  • 304
    • 0028222730 scopus 로고
    • Verongamine, a novel bromotyrosinederived histamine H3-antagonist from the marine sponge Verongula gigantean
    • Mierzwa, R., King, A., Conover, M.A. et al. 1994. Verongamine, a novel bromotyrosinederived histamine H3-antagonist from the marine sponge Verongula gigantean. J. Nat. Prod. 57: 175-177.
    • (1994) J. Nat. Prod , vol.57 , pp. 175-177
    • Mierzwa, R.1    King, A.2    Conover, M.A.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.