@article{b2b763b77e584f498b4803eda43c0375,
title = "TRPV1 antagonist with high analgesic efficacy: 2-Thio pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides",
abstract = "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.",
keywords = "Analgesic, Capsaicin, Resiniferatoxin, TRPV1 antagonists",
author = "Ha, {Tae Hwan} and Hyungchul Ryu and Kim, {Sung Eun} and Kim, {Ho Shin} and Jihyae Ann and Tran, {Phuong Thao} and Hoang, {Van Hai} and Karam Son and Minghua Cui and Sun Choi and Blumberg, {Peter M.} and Robert Frank and Gregor Bahrenberg and Klaus Schiene and Thomas Christoph and Sven Frormann and Jeewoo Lee",
note = "Funding Information: This research was supported by Research Grants from Grunenthal, Grants from the National Research Foundation of Korea (NRF) ( R11-2007-107-02001-0 ), Grants from the National Leading Research Lab (NLRL) program ( 2011-0028885 ), and in part by the Intramural Research Program of NIH, Center for Cancer Research, NCI (Project Z1A BC 005270 ).",
year = "2013",
month = nov,
day = "1",
doi = "10.1016/j.bmc.2013.08.015",
language = "English",
volume = "21",
pages = "6657--6664",
journal = "Bioorganic and Medicinal Chemistry",
issn = "0968-0896",
publisher = "Elsevier Ltd.",
number = "21",
}