메뉴 건너뛰기




Volumn 55, Issue 21, 2012, Pages 9240-9254

Identification of multiple 5-HT4 partial agonist clinical candidates for the treatment of alzheimers disease

Author keywords

[No Author keywords available]

Indexed keywords

4 [4 [(TETRAHYDROFURAN 3 YL)OXY]BENZO[D]ISOXAZOL 4 YLOXYMETHYL]PIPERIDIN 1 YLMETHYL]TETRAHYDROPYRAN 4 OL; 6 FLUORO 3,3 DIMETHYL 2 OXO 2,3 DIHYDROINDOLE 1 CARBOXYLIC ACID [1 (4 HYDROXYTETRAHYDROPYRAN 4 YLMETHYL)PIPERIDIN 4 YLMETHYL]AMIDE; 6 FLUORO N [[1 [(4 HYDROXYTETRAHYDRO 2H PYRAN 4 YL)METHYL]PIPERIDIN 4 YL]METHYL] 3 ISOPROPYL 2 OXO 2,3 DIHYDRO 1H BENZO[D]IMIDAZOLE 1 CARBOXAMIDE; PARTIAL AGONIST; SEROTONIN 4 AGONIST; SEROTONIN 4 RECEPTOR; UNCLASSIFIED DRUG;

EID: 84868576372     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm300953p     Document Type: Article
Times cited : (38)

References (33)
  • 1
    • 84860618647 scopus 로고    scopus 로고
    • The growing burden of Alzheimers disease
    • Lopez, O. L. The growing burden of Alzheimers disease Am. J. Managed Care 2011, 17 (Suppl. 13) S339-S345
    • (2011) Am. J. Managed Care , vol.17 , Issue.SUPPL. 13
    • Lopez, O.L.1
  • 2
    • 84858225391 scopus 로고    scopus 로고
    • 2012 Alzheimers disease facts and figures
    • 2012 Alzheimers disease facts and figures. Alzheimer's Dementia 2012, 8 (2), 131-168.
    • (2012) Alzheimer's Dementia , vol.8 , Issue.2 , pp. 131-168
  • 3
    • 77949335521 scopus 로고    scopus 로고
    • The worldwide societal costs of dementia: Estimates for 2009
    • Wimo, A.; Winblad, B.; Jonsson, L. The worldwide societal costs of dementia: estimates for 2009 Alzheimer's Dementia 2010, 6 (2) 98-103
    • (2010) Alzheimer's Dementia , vol.6 , Issue.2 , pp. 98-103
    • Wimo, A.1    Winblad, B.2    Jonsson, L.3
  • 4
    • 0019972810 scopus 로고
    • The cholinergic hypothesis of geriatric memory dysfunction
    • Bartus, R. T.; Dean, R. L., 3rd; Beer, B.; Lippa, A. S. The cholinergic hypothesis of geriatric memory dysfunction Science 1982, 217 (4558) 408-414
    • (1982) Science , vol.217 , Issue.4558 , pp. 408-414
    • Bartus, R.T.1    Dean III, R.L.2    Beer, B.3    Lippa, A.S.4
  • 7
    • 0028177450 scopus 로고
    • 5-HT4 receptor stimulation facilitates acetylcholine release in rat frontal cortex
    • Consolo, S.; Arnaboldi, S.; Giorgi, S.; Russi, G.; Ladinsky, H. 5-HT4 receptor stimulation facilitates acetylcholine release in rat frontal cortex NeuroReport 1994, 5 (10) 1230-1232
    • (1994) NeuroReport , vol.5 , Issue.10 , pp. 1230-1232
    • Consolo, S.1    Arnaboldi, S.2    Giorgi, S.3    Russi, G.4    Ladinsky, H.5
  • 9
    • 0029956067 scopus 로고    scopus 로고
    • Stereoselective effects of (R)- and (S)-zacopride on cognitive performance in a spatial navigation task in rats
    • Fontana, D. J.; Daniels, S. E.; Eglen, R. M.; Wong, E. H. Stereoselective effects of (R)- and (S)-zacopride on cognitive performance in a spatial navigation task in rats Neuropharmacology 1996, 35 (3) 321-327
    • (1996) Neuropharmacology , vol.35 , Issue.3 , pp. 321-327
    • Fontana, D.J.1    Daniels, S.E.2    Eglen, R.M.3    Wong, E.H.4
  • 10
    • 0032158693 scopus 로고    scopus 로고
    • Role of 5-HT4 receptors in the mouse passive avoidance test
    • Galeotti, N.; Ghelardini, C.; Bartolini, A. Role of 5-HT4 receptors in the mouse passive avoidance test J. Pharmacol. Exp. Ther. 1998, 286 (3) 1115-1121
    • (1998) J. Pharmacol. Exp. Ther. , vol.286 , Issue.3 , pp. 1115-1121
    • Galeotti, N.1    Ghelardini, C.2    Bartolini, A.3
  • 13
    • 77953680038 scopus 로고    scopus 로고
    • Defining desirable central nervous system drug space through the alignment of molecular properties, in vitro ADME, and safety attributes
    • Wager, T. T.; Chandrasekaran, R. Y.; Hou, X.; Troutman, M. D.; Verhoest, P. R.; Villalobos, A.; Will, Y. Defining desirable central nervous system drug space through the alignment of molecular properties, in vitro ADME, and safety attributes ACS Chem. Neurosci. 2010, 1 (6) 420-434
    • (2010) ACS Chem. Neurosci. , vol.1 , Issue.6 , pp. 420-434
    • Wager, T.T.1    Chandrasekaran, R.Y.2    Hou, X.3    Troutman, M.D.4    Verhoest, P.R.5    Villalobos, A.6    Will, Y.7
  • 18
    • 38749087222 scopus 로고    scopus 로고
    • In vitro P-glycoprotein assays to predict the in vivo interactions of P-glycoprotein with drugs in the central nervous system
    • Feng, B.; Mills, J. B.; Davidson, R. E.; Mireles, R. J.; Janiszewski, J. S.; Troutman, M. D.; de Morais, S. M. In vitro P-glycoprotein assays to predict the in vivo interactions of P-glycoprotein with drugs in the central nervous system Drug Metab. Dispos. 2008, 36 (2) 268-275
    • (2008) Drug Metab. Dispos. , vol.36 , Issue.2 , pp. 268-275
    • Feng, B.1    Mills, J.B.2    Davidson, R.E.3    Mireles, R.J.4    Janiszewski, J.S.5    Troutman, M.D.6    De Morais, S.M.7
  • 19
    • 0036874825 scopus 로고    scopus 로고
    • Influence of nonspecific brain and plasma binding on CNS exposure: Implications for rational drug discovery
    • Kalvass, J. C.; Maurer, T. S. Influence of nonspecific brain and plasma binding on CNS exposure: implications for rational drug discovery Biopharm. Drug Dispos. 2002, 23 (8) 327-338
    • (2002) Biopharm. Drug Dispos. , vol.23 , Issue.8 , pp. 327-338
    • Kalvass, J.C.1    Maurer, T.S.2
  • 20
    • 84875003842 scopus 로고    scopus 로고
    • version 6; ICON: Columbia, MD
    • The following software was utilized: NONMEM, version 6; ICON: Columbia, MD.
    • NONMEM
  • 21
    • 47749097152 scopus 로고    scopus 로고
    • Contribution of active and inactive states of the human 5-HT4d receptor to the functional activities of 5-HT4-receptor agonists
    • Mikami, T.; Sugimoto, H.; Naganeo, R.; Ohmi, T.; Saito, T.; Eda, H. Contribution of active and inactive states of the human 5-HT4d receptor to the functional activities of 5-HT4-receptor agonists J. Pharmacol. Sci. 2008, 107 (3) 251-259
    • (2008) J. Pharmacol. Sci. , vol.107 , Issue.3 , pp. 251-259
    • Mikami, T.1    Sugimoto, H.2    Naganeo, R.3    Ohmi, T.4    Saito, T.5    Eda, H.6
  • 22
    • 0031870681 scopus 로고    scopus 로고
    • Comparative 5-HT4 receptor antagonist activity of LY353433 and its active hydroxylated metabolites
    • Cohen, M. L.; Bloomquist, W.; Calligaro, D.; Swanson, S. Comparative 5-HT4 receptor antagonist activity of LY353433 and its active hydroxylated metabolites Drug Dev. Res. 1998, 43 (4) 193-199
    • (1998) Drug Dev. Res. , vol.43 , Issue.4 , pp. 193-199
    • Cohen, M.L.1    Bloomquist, W.2    Calligaro, D.3    Swanson, S.4
  • 23
    • 0037472231 scopus 로고    scopus 로고
    • 5-HT4 receptor ligands: Applications and new prospects
    • Langlois, M.; Fischmeister, R. 5-HT4 receptor ligands: applications and new prospects J. Med. Chem. 2003, 46 (3) 319-344
    • (2003) J. Med. Chem. , vol.46 , Issue.3 , pp. 319-344
    • Langlois, M.1    Fischmeister, R.2
  • 24
    • 0035894575 scopus 로고    scopus 로고
    • Serotoninergic neuroenteric modulators
    • Talley, N. J. Serotoninergic neuroenteric modulators Lancet 2001, 358 (9298) 2061-2068
    • (2001) Lancet , vol.358 , Issue.9298 , pp. 2061-2068
    • Talley, N.J.1
  • 25
    • 24044443262 scopus 로고    scopus 로고
    • Prucalopride is a partial agonist through human and porcine atrial 5-HT4 receptors: Comparison with recombinant human 5-HT4 splice variants
    • Krobert, K. A.; Brattelid, T.; Levy, F. O.; Kaumann, A. J. Prucalopride is a partial agonist through human and porcine atrial 5-HT4 receptors: comparison with recombinant human 5-HT4 splice variants Naunyn Schmiedeberg's Arch. Pharmacol. 2005, 371 (6) 473-479
    • (2005) Naunyn Schmiedeberg's Arch. Pharmacol. , vol.371 , Issue.6 , pp. 473-479
    • Krobert, K.A.1    Brattelid, T.2    Levy, F.O.3    Kaumann, A.J.4
  • 26
    • 67349097389 scopus 로고    scopus 로고
    • Target site occupancy: Emerging generalizations from clinical and preclinical studies
    • Grimwood, S.; Hartig, P. R. Target site occupancy: emerging generalizations from clinical and preclinical studies Pharmacol. Ther. 2009, 122 (3) 281-301
    • (2009) Pharmacol. Ther. , vol.122 , Issue.3 , pp. 281-301
    • Grimwood, S.1    Hartig, P.R.2
  • 27
    • 0030955397 scopus 로고    scopus 로고
    • The effects of novel, selective 5-hydroxytryptamine (5-HT)4 receptor ligands in rat spatial navigation
    • Fontana, D. J.; Daniels, S. E.; Wong, E. H.; Clark, R. D.; Eglen, R. M. The effects of novel, selective 5-hydroxytryptamine (5-HT)4 receptor ligands in rat spatial navigation Neuropharmacology 1997, 36 (4-5) 689-696
    • (1997) Neuropharmacology , vol.36 , Issue.4 , pp. 689-696
    • Fontana, D.J.1    Daniels, S.E.2    Wong, E.H.3    Clark, R.D.4    Eglen, R.M.5
  • 28
    • 0021173996 scopus 로고
    • Developments of a water-maze procedure for studying spatial learning in the rat
    • Morris, R. Developments of a water-maze procedure for studying spatial learning in the rat J. Neurosci. Methods 1984, 11 (1) 47-60
    • (1984) J. Neurosci. Methods , vol.11 , Issue.1 , pp. 47-60
    • Morris, R.1
  • 29
    • 0032733974 scopus 로고    scopus 로고
    • Prediction of human clearance of twenty-nine drugs from hepatic microsomal intrinsic clearance data: An examination of in vitro half-life approach and nonspecific binding to microsomes
    • Obach, R. S. Prediction of human clearance of twenty-nine drugs from hepatic microsomal intrinsic clearance data: an examination of in vitro half-life approach and nonspecific binding to microsomes Drug Metab. Dispos. 1999, 27 (11) 1350-1359
    • (1999) Drug Metab. Dispos. , vol.27 , Issue.11 , pp. 1350-1359
    • Obach, R.S.1
  • 30
    • 0034676533 scopus 로고    scopus 로고
    • Asymmetric synthesis of the fully functional macrolide core of salicylihalamide: Remote control of olefin geometry during RCM
    • Furstner, A.; Thiel, O. R.; Blanda, G. Asymmetric synthesis of the fully functional macrolide core of salicylihalamide: remote control of olefin geometry during RCM Org. Lett. 2000, 2 (23) 3731-3734
    • (2000) Org. Lett. , vol.2 , Issue.23 , pp. 3731-3734
    • Furstner, A.1    Thiel, O.R.2    Blanda, G.3
  • 32
    • 0033614953 scopus 로고    scopus 로고
    • 2,3-Dihydro-2-oxo-1 H -benzimidazole-1-carboxamides with selective affinity for the 5-HT(4) receptor: Synthesis and structure-affinity and structure-activity relationships of a new series of partial agonist and antagonist derivatives
    • Tapia, I.; Alonso-Cires, L.; Lopez-Tudanca, P. L.; Mosquera, R.; Labeaga, L.; Innerarity, A.; Orjales, A. 2,3-Dihydro-2-oxo-1 H -benzimidazole-1- carboxamides with selective affinity for the 5-HT(4) receptor: synthesis and structure-affinity and structure-activity relationships of a new series of partial agonist and antagonist derivatives J. Med. Chem. 1999, 42 (15) 2870-2880
    • (1999) J. Med. Chem. , vol.42 , Issue.15 , pp. 2870-2880
    • Tapia, I.1    Alonso-Cires, L.2    Lopez-Tudanca, P.L.3    Mosquera, R.4    Labeaga, L.5    Innerarity, A.6    Orjales, A.7
  • 33
    • 0003633755 scopus 로고    scopus 로고
    • Institute of Laboratory Animal Resources. National Institutes of Health Publication 85-23; National Academy Press: Washington, DC
    • Animal use reference: Institute of Laboratory Animal Resources. Guide for the Care and Use of Laboratory Animals; National Institutes of Health Publication 85-23; National Academy Press: Washington, DC, 1996.
    • (1996) Guide for the Care and Use of Laboratory Animals


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.