Referenced in: none

Automatically associated channels: TRP , TRPV , TRPV1

Title: Heterocycle-linked phenylbenzyl amides as novel TRPV1 antagonists and their TRPV1 binding modes: constraint-induced enhancement of in vitro and in vivo activities.

Authors: Nam-Jung Kim, Fu-Nan Li, Jin Hee Lee, Seul-Gi Park, Kyeojin Kim, Changjin Lim, Young Taek Han, Hwayoung Yun, Jong-Wha Jung, Hyeung-Geun Park, Hee-Doo Kim, Byoung Young Woo, Song Seok Shin, Sun-Young Kim, Jin Kyu Choi, Yeon-Su Jeong, Yanghui Park, Young-Ho Park, Dae-Duk Kim, Sun Choi, Young-Ger Suh

Journal, date & volume: Chem Asian J, 2013 Feb , 8, 400-9

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/23208797

Abstract
A series of heterocycle-linked constrained phenylbenzyl amides were found to be TRPV1 antagonists with promising in vivo profiles. In particular, one of the analogues containing a furan linker exhibited excellent TRPV1 antagonistic activity and in vivo analgesic efficacy. In addition, the binding modes of dibenzyl thiourea, benzylphenethyl amide, and furan-linked phenylbenzyl amide were examined by using the flexible docking study within the rTRPV1 homology model.