582325-38-0Relevant articles and documents
4-(2-Pyridyl)piperazine-1-benzimidazoles as potent TRPV1 antagonists
Shao, Bin,Huang, Jincheng,Sun, Qun,Valenzano, Kenneth J.,Schmid, Lori,Nolan, Scott
, p. 719 - 723 (2005)
A series of 4-(2-pyridyl)piperazine-1-benzimidazole analogues based on compound 1 was synthesized and evaluated for TRPV1 antagonist activity in capsaicin-induced (CAP) and pH 5.5-induced (pH) FLIPR assays in a human TRPV1-expressing HEK293 cell line. Potent TRPV1 antagonists were identified through SAR studies. From these studies, several antagonists were found, with IC50 values ranging from 32 nM to ~5000 nM. Among these, 11 [IC50 = 90 nM (CAP) and 104 nM (pH)] was further evaluated and found to be orally available in rats (F% = 19.7).