Nonpeptide angiotensin II antagonists derived from 1H-pyrazole-5-carboxylates and 4-aryl-1H-imidazole-5-carboxylates
作者:Wallace T. Ashton、Steven M. Hutchins、William J. Greenlee、George A. Doss、Raymond S. L. Chang、Victor J. Lotti、Kristie A. Faust、Tsing Bau Chen、Gloria J. Zingaro
DOI:10.1021/jm00075a014
日期:1993.11
phenyl)-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-y l] methyl]-1H-imidazole-5-carboxylic acid (12b), which was found to be a highly potent antagonist of the rabbit aorta AT1 receptor (IC50 0.55 nM). In conscious, normotensive rats, 12b at 0.1 mg/kg iv inhibited the pressor response to AII by 88%, with a duration of > 6 h. More extensively studied was an isosteric series of 3-alkyl-4-[[2'-(1H-tetrazol-5-
Synthesis, Opioid Receptor Binding, and Bioassay of Naltrindole Analogues Substituted in the Indolic Benzene Moiety
作者:Subramaniam Ananthan、Cheryl A. Johnson、Ronald L. Carter、Sarah D. Clayton、Kenner C. Rice、Heng Xu、Peg Davis、Frank Porreca、Richard B. Rothman
DOI:10.1021/jm980083i
日期:1998.7.1
assays in rat or guinea pig brain membranes and for their opioid antagonist and agonist activities in vitro on the guinea pig ileum (GPI) and mouse vas deferens (MVD) preparations. All of the compounds displayed delta selectivity in binding to the delta, mu, and kappa opioidreceptors. The binding potencies of most of the compounds at the delta, mu, and kappa sites, however, were lower than that of 1. Among
Buu-Hoi et al., Recueil des Travaux Chimiques des Pays-Bas, 1950, vol. 69, p. 1053,1078
作者:Buu-Hoi et al.
DOI:——
日期:——
[EN] HETEROCYCLIC MODULATORS OF GPR119 FOR TREATMENT OF DISEASE<br/>[FR] MODULATEURS HÉTÉROCYCLIQUES DE GPR119 POUR LE TRAITEMENT D'UNE MALADIE
申请人:KALYPSYS INC
公开号:WO2009117421A2
公开(公告)日:2009-09-24
The present invention relates to compounds and methods which may be useful as inhibitors of GPR119 for the treatment or prevention of metabolic, cardiovascular, and metabolic diseases.