PubMed 24035514

Referenced in Channelpedia wiki pages of: none

Automatically associated channels: TRP , TRPV , TRPV1

Title: TRPV1 antagonist with high analgesic efficacy: 2-Thio pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides.

Authors: Tae-Hwan Ha, HyungChul Ryu, Sung-Eun Kim, Ho Shin Kim, Jihyae Ann, Phuong-Thao Tran, Van-Hai Hoang, Karam Son, Minghua Cui, Sun Choi, Peter M Blumberg, Robert Frank, Gregor Bahrenberg, Klaus Schiene, Thomas Christoph, Sven Frormann, Jeewoo Lee

Journal, date & volume: Bioorg. Med. Chem., 2013 Nov 1 , 21, 6657-64

PubMed link:

A series of 2-thio pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides were investigated as hTRPV1 antagonists. Among them, compound 24S showed stereospecific and excellent TRPV1 antagonism of capsaicin-induced activation. Further, it demonstrated strong anti-allodynic in a rat neuropathic pain model. Consistent with its action in vitro being through TRPV1, compound 24S blocked capsaicin-induced hypothermia in mice. Docking analysis of 24S with our hTRPV1 homology model was performed to identify its binding mode.