Referenced in: none

Automatically associated channels: Kir2.3 , TRP , TRPV , TRPV1

Title: α-Methylated simplified resiniferatoxin (sRTX) thiourea analogues as potent and stereospecific TRPV1 antagonists.

Authors: Ho Shin Kim, Mi-Kyoung Jin, Sang-Uk Kang, Ju-Ok Lim, Phuong-Thao Tran, Van-Hai Hoang, Jihyae Ann, Tae-Hwan Ha, Larry V Pearce, Vladimir A Pavlyukovets, Peter M Blumberg, Jeewoo Lee

Journal, date & volume: Bioorg. Med. Chem. Lett., 2014 Jun 15 , 24, 2685-8

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/24794110

Abstract
A series of α-methylated analogues of the potent sRTX thiourea antagonists were investigated as rTRPV1 ligands in order to examine the effect of α-methylation on receptor activity. The SAR analysis indicated that activity was stereospecific with the (R)-configuration of the newly formed chiral center providing high binding affinity and potent antagonism while the configuration of the C-region was not significant.