PubMed 25011915

Referenced in Channelpedia wiki pages of: none

Automatically associated channels: TRP , TRPV , TRPV1

Title: 2-Aryl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists.

Authors: HyungChul Ryu, Sejin Seo, Myeong Seop Kim, Mi-Yeon Kim, Ho Shin Kim, Jihyae Ann, Phuong-Thao Tran, Van-Hai Hoang, Jieun Byun, Minghua Cui, Karam Son, Pankaz Kumar Sharma, Sun Choi, Peter M Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Babette-Yvonne Koegel, Thomas Christoph, Sven Frormann, Jeewoo Lee

Journal, date & volume: Bioorg. Med. Chem. Lett., 2014 Aug 15 , 24, 4044-7

PubMed link:

A series of 2-aryl pyridine C-region derivatives of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides were investigated as hTRPV1 antagonists. Multiple compounds showed highly potent TRPV1 antagonism toward capsaicin comparable to previous lead 7. Among them, compound 9 demonstrated anti-allodynia in a mouse neuropathic pain model and blocked capsaicin-induced hypothermia in a dose-dependent manner. Docking analysis of 9 with our hTRPV1 homology model provided insight into its specific binding mode.