736971-00-9Relevant articles and documents
Synthesis and evaluation of thiazole carboxamides as vanilloid receptor 1 (TRPV1) antagonists
Xi, Ning,Bo, Yunxin,Doherty, Elizabeth M.,Fotsch, Christopher,Gavva, Narender R.,Han, Nianhe,Hungate, Randall W.,Klionsky, Lana,Liu, Qingyian,Tamir, Rami,Xu, Shimin,Treanor, James J.S.,Norman, Mark H.
, p. 5211 - 5217 (2007/10/03)
A thiazole derivative, 2-(2,6-dichlorobenzyl)-N-(4-isopropylphenyl) thiazole-4-carboxamide (1), was identified as a TRPV1 antagonist. We synthesized various thiazole analogs and evaluated them for their ability to block capsaicin- or acid-induced calcium influx in TRPV1-expressing CHO cells. The IC50 values of the most potent antagonists were ca. 0.050 μM in these assays.
