Referenced in: none

Automatically associated channels: TRP , TRPV , TRPV1

Title: The SAR analysis of TRPV1 agonists with the α-methylated B-region.

Authors: Yongsung Cho, Myeong Seop Kim, Ho Shin Kim, Jihyae Ann, Jiyoun Lee, Larry V Pearce, Vladimir A Pavlyukovets, Matthew A Morgan, Peter M Blumberg, Jeewoo Lee

Journal, date & volume: Bioorg. Med. Chem. Lett., 2012 Aug 15 , 22, 5227-31

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/22796184

Abstract
A series of TRPV1 agonists with amide, reverse amide, and thiourea groups in the B-region and their corresponding α-methylated analogues were investigated. Whereas the α-methylation of the amide B-region enhanced the binding affinities and potencies as agonists, that of the reverse amide and thiourea led to a reduction in receptor affinity. The analysis indicated that proper hydrogen bonding as well as steric effects in the B-region are critical for receptor binding.