메뉴 건너뛰기




Volumn 46, Issue 26, 2003, Pages 5567-5570

Synthesis, in Vitro Affinity, and Efficacy of a Bis 8-Ethynyl-4H-imidazo[1,5a]-[1,4]benzodiazepine Analogue, the First Bivalent α5 Subtype Selective BzR/GABAA Antagonist

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR BLOCKING AGENT; BENZODIAZEPINE DERIVATIVE; BENZODIAZEPINE RECEPTOR; BIS 8 ETHYNYL 4H IMIDAZO[1,5][1,4]BENZODIAZEPINE DERIVATIVE; DIAZEPAM; LIGAND; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG;

EID: 0347627160     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm034164c     Document Type: Article
Times cited : (47)

References (32)
  • 1
    • 0017614063 scopus 로고
    • Benzodiazepine Receptors in Rat Brain
    • Squires, R. F.; Braestrup, C. Benzodiazepine Receptors in Rat Brain. Nature 1977, 266, 732-734.
    • (1977) Nature , vol.266 , pp. 732-734
    • Squires, R.F.1    Braestrup, C.2
  • 2
    • 0028981088 scopus 로고
    • A Receptor Subtypes
    • A Receptor Subtypes. Pharm. Rev. 1995, 47, 181-234.
    • (1995) Pharm. Rev. , vol.47 , pp. 181-234
    • Sieghart, W.1
  • 4
    • 0031799363 scopus 로고    scopus 로고
    • International Union of Pharmacology. XV. Subtypes of γ -Aminobutyric AcidA Receptors: Classification on the Basis of Subunit Structure and Receptor Function
    • Barnard, E. A.; Skolnick, P.; Olsen, R. W.; Möhler, H.; Sieghart, W.; Biggio, G.; Braestrup, C.; Bateson, A. N.; Langer, S. Z. International Union of Pharmacology. XV. Subtypes of γ-Aminobutyric AcidA Receptors: Classification on the Basis of Subunit Structure and Receptor Function. Pharmcol. Rev. 1998, 50, 291-313.
    • (1998) Pharmcol. Rev. , vol.50 , pp. 291-313
    • Barnard, E.A.1    Skolnick, P.2    Olsen, R.W.3    Möhler, H.4    Sieghart, W.5    Biggio, G.6    Braestrup, C.7    Bateson, A.N.8    Langer, S.Z.9
  • 9
    • 0026612363 scopus 로고
    • A Receptor Subunit mRNAs in the Rat Brain. I. Telencephalon, Diencephalon, Mesencephalon
    • A Receptor Subunit mRNAs in the Rat Brain. I. Telencephalon, Diencephalon, Mesencephalon. J. Neurosci. 1992, 12, 1040-1062.
    • (1992) J. Neurosci. , vol.12 , pp. 1040-1062
    • Wisden, W.1    Laurie, D.J.2    Monyer, H.3    Seeburg, P.H.4
  • 15
    • 0002926929 scopus 로고    scopus 로고
    • A/Benzodiazepine Receptor Subsites. Potent Affinities of the (S)-Enantiomers of Framework-Constrained 4,5-Substituted Pyrroloimidazobenzodiazepines
    • A/Benzodiazepine Receptor Subsites. Potent Affinities of the (S)-Enantiomers of Framework-Constrained 4,5-Substituted Pyrroloimidazobenzodiazepines. Med. Chem. Res. 1997, 7, 25-35.
    • (1997) Med. Chem. Res. , vol.7 , pp. 25-35
    • Liu, R.1    Zhang, P.2    Gan, T.3    McKernan, R.M.4    Cook, J.M.5
  • 16
    • 0000676605 scopus 로고    scopus 로고
    • Benzo-Fused Benzodiazepines Employed as Topological Probes for the Study of Benzodiazepine Receptor Subtypes
    • Huang, Q.; Zhang, W.; Liu, R.; McKernan, R. M.; Cook, J. M. Benzo-Fused Benzodiazepines Employed as Topological Probes for the Study of Benzodiazepine Receptor Subtypes. Med. Chem. Res. 1996, 6, 384-391.
    • (1996) Med. Chem. Res. , vol.6 , pp. 384-391
    • Huang, Q.1    Zhang, W.2    Liu, R.3    McKernan, R.M.4    Cook, J.M.5
  • 18
    • 0031783661 scopus 로고    scopus 로고
    • Rat and Human Hippocampal α5 Subunit-Containing γ-Aminobutyric AcidA Receptors Have α5β3γ2 Pharmacological Characteristics
    • Sur, C.; Quirk, K.; Dewar, D.; Atack, J. R.; McKernan, R. Rat and Human Hippocampal α5 Subunit-Containing γ-Aminobutyric AcidA Receptors Have α5β3γ2 Pharmacological Characteristics. Mol Pharmacol. 1998, 54, 928-933.
    • (1998) Mol Pharmacol. , vol.54 , pp. 928-933
    • Sur, C.1    Quirk, K.2    Dewar, D.3    Atack, J.R.4    McKernan, R.5
  • 19
    • 0036292157 scopus 로고    scopus 로고
    • Effects of Hippocampal Injections of a Novel Ligand Selective for the α5β2γ2 Subunits of the GABA/Benzodiazepine Receptor on Pavlovian Conditioning
    • Bailey, D. J.; Tetzlaff, J. E.; Cook, J. M.; He, X.; Helmstetter, F. J. Effects of Hippocampal Injections of a Novel Ligand Selective for the α5β2γ2 Subunits of the GABA/Benzodiazepine Receptor on Pavlovian Conditioning. Neurobiol. Learning Memory 2002, 78, 1-10.
    • (2002) Neurobiol. Learning Memory , vol.78 , pp. 1-10
    • Bailey, D.J.1    Tetzlaff, J.E.2    Cook, J.M.3    He, X.4    Helmstetter, F.J.5
  • 20
    • 0035943336 scopus 로고    scopus 로고
    • Influence of Benzodiazepine Binding Site Ligands on Fear-Conditioned Contextual Memory
    • DeLorey, T.; Lin, R.; McBrad, B.; He, X.; Cook, J. M.; Lameh, J.; Loew, G. Influence of Benzodiazepine Binding Site Ligands on Fear-Conditioned Contextual Memory. Eur. J. Pharmacol. 2001, 426, 45-54.
    • (2001) Eur. J. Pharmacol. , vol.426 , pp. 45-54
    • DeLorey, T.1    Lin, R.2    McBrad, B.3    He, X.4    Cook, J.M.5    Lameh, J.6    Loew, G.7
  • 21
    • 0025992652 scopus 로고
    • Taking Stock of Cognition Enhancers
    • Sarter, M. Taking Stock of Cognition Enhancers. Trends Pharmacol. Sci. Rev. 1991, 12, 456-461.
    • (1991) Trends Pharmacol. Sci. Rev. , vol.12 , pp. 456-461
    • Sarter, M.1
  • 22
    • 0032961958 scopus 로고    scopus 로고
    • G-Protein Coupled Receptors, Bivalent Ligands and Drug Design
    • Halazy, S. G-Protein Coupled Receptors, Bivalent Ligands and Drug Design. In Exp. Opin. Ther. Pat. 9, 1999, 431-446.
    • (1999) Exp. Opin. Ther. Pat. , vol.9 , pp. 431-446
    • Halazy, S.1
  • 23
    • 0024405504 scopus 로고
    • Bivalent Ligands and the Message-Address Concept in the Design of Selective Opioid Receptor Antagonists
    • Portoghese, P. Bivalent Ligands and the Message-Address Concept in the Design of Selective Opioid Receptor Antagonists. Trends Pharmacol. Sci. 1989, 10, 230-235.
    • (1989) Trends Pharmacol. Sci. , vol.10 , pp. 230-235
    • Portoghese, P.1
  • 24
    • 0028275934 scopus 로고
    • Structure-Activity Relationship of N17′-Substituted Norbinaltorphimine Congeners. Role of the N17′ Basic Group in the Interaction with a Putative Address Subsite on the Kappa Opioid Receptor
    • Portoghese, P.; Lin, C.; Farouz-Grant, F.; Takemori, A. E. Structure-Activity Relationship of N17′-Substituted Norbinaltorphimine Congeners. Role of the N17′ Basic Group in the Interaction with a Putative Address Subsite on the Kappa Opioid Receptor. J. Med. Chem. 1994, 37, 1495-1500.
    • (1994) J. Med. Chem. , vol.37 , pp. 1495-1500
    • Portoghese, P.1    Lin, C.2    Farouz-Grant, F.3    Takemori, A.E.4
  • 25
    • 0001584789 scopus 로고
    • Quinazolines and 1,4-Benzodiazepines. XVII. Synthesis of 1,3-Dihydro-5-Pyridyl-2H-1,4-Benzodiazepine Derivatives
    • Fryer, R. I.; Schmidt, R. A.; Sternbach, L. H. Quinazolines and 1,4-Benzodiazepines. XVII. Synthesis of 1,3-Dihydro-5-Pyridyl-2H-1,4-Benzodiazepine Derivatives. J. Pharm. Sci. 1964, 53, 264-268.
    • (1964) J. Pharm. Sci. , vol.53 , pp. 264-268
    • Fryer, R.I.1    Schmidt, R.A.2    Sternbach, L.H.3
  • 26
    • 0007501031 scopus 로고
    • Conformational Similarity of Diazepam-Sensitive and -Insensitive Benzodiazepine Receptors Determined by Chiral Pyrroloimidazobenzodiazepines
    • Fryer, R. I.; Zhang, P.; Lin, K.-Y.; Upasani, R. B.; Wong, G.; Skolnick, P. Conformational Similarity of Diazepam-Sensitive and -Insensitive Benzodiazepine Receptors Determined by Chiral Pyrroloimidazobenzodiazepines. Med. Chem. Res. 1993, 3, 183-191.
    • (1993) Med. Chem. Res. , vol.3 , pp. 183-191
    • Fryer, R.I.1    Zhang, P.2    Lin, K.-Y.3    Upasani, R.B.4    Wong, G.5    Skolnick, P.6
  • 27
    • 0026341843 scopus 로고
    • Synthesis of Novel Substituted 4H-Imidazo [1,5-α ][1,4]-Benzodiazepines
    • Fryer, R. I.; Gu, Z. Q.; Wang, C. G. Synthesis of Novel Substituted 4H-Imidazo [1,5-α][1,4]-Benzodiazepines. J. Heterocycl. Chem. 1991, 28, 1661-1669.
    • (1991) J. Heterocycl. Chem. , vol.28 , pp. 1661-1669
    • Fryer, R.I.1    Gu, Z.Q.2    Wang, C.G.3
  • 28
    • 0028912677 scopus 로고
    • Development of a Comprehensive Pharmacophore Model for the Benzodiazepine Receptor
    • Zhang, W.; Koehler, K. F.; Zhang, P.; Cook, J. M. Development of a Comprehensive Pharmacophore Model for the Benzodiazepine Receptor. Drug Des. Discovery 1995, 12, 193-248.
    • (1995) Drug Des. Discovery , vol.12 , pp. 193-248
    • Zhang, W.1    Koehler, K.F.2    Zhang, P.3    Cook, J.M.4
  • 30
    • 0033776741 scopus 로고    scopus 로고
    • Pharmacophore/Receptor Models for GABA/BzR α2β3γ2, α3β3 γ2 and α4β3γ2 Recombinant Subtypes. Included Volume Analysis and Comparison to α1β3γ2, α5β3γ2 and α6β3γ2 Subtypes
    • He, X.; Huang, Q.; Ma, C.; Yu, S.; McKernan, R.; Cook, J. M. Pharmacophore/Receptor Models for GABA/BzR α2β3γ2, α3β3 γ2 and α4β3γ2 Recombinant Subtypes. Included Volume Analysis and Comparison to α1β3γ2, α5β3γ2 and α6β3γ2 Subtypes. Drug Des. Discovery 2000, 17, 131-171.
    • (2000) Drug Des. Discovery , vol.17 , pp. 131-171
    • He, X.1    Huang, Q.2    Ma, C.3    Yu, S.4    McKernan, R.5    Cook, J.M.6
  • 32
    • 0036196828 scopus 로고    scopus 로고
    • Tranexamic Acid, a Widely Used Antifibrinolytic Agent, Causes Convulsions by a Gamma-aminobutyric Acid(A) Receptor Antagonistic Effect
    • Furtmuller, R.; Schlag, M. G.; Berger, M.; Hopf, R.; Huck, S.; Sieghart, W.; Redl, H. Tranexamic Acid, a Widely Used Antifibrinolytic Agent, Causes Convulsions by a Gamma-aminobutyric Acid(A) Receptor Antagonistic Effect. J. Pharmacol. Exp. Ther. 2002, 301(1), 168-173.
    • (2002) J. Pharmacol. Exp. Ther. , vol.301 , Issue.1 , pp. 168-173
    • Furtmuller, R.1    Schlag, M.G.2    Berger, M.3    Hopf, R.4    Huck, S.5    Sieghart, W.6    Redl, H.7


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.