Author/Authors :
Ning Xi، نويسنده , , Yunxin Bo، نويسنده , , Elizabeth M. Doherty، نويسنده , , Christopher Fotsch، نويسنده , , Narender R. Gavva، نويسنده , , Nianhe Han، نويسنده , , Randall W. Hungate، نويسنده , , Lana Klionsky، نويسنده , , Qingyian Liu، نويسنده , , Rami Tamir، نويسنده , , Shimin Xu، نويسنده , , James J.S. Treanor، نويسنده , , Mark H. Norman، نويسنده ,
Abstract :
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.
