@article{3c4bee12d1904e319e9bb42bb6c3256a,
title = "Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic",
abstract = "Paradoxically, some TRPV1 agonists are, at the organismal level, both nonpungent and clinically useful as topical analgesics. Here, we describe the scaled-up synthesis and characterization in mouse models of a novel, nonpungent vanilloid. Potent analgesic activity was observed in models of neuropathic pain, and the compound blocked capsaicin induced allodynia, showing dermal accumulation with little transdermal absorption. Finally, it displayed much weaker systemic toxicity compared to capsaicin and was negative in assays of genotoxicity.",
author = "Jihyae Ann and Kim, {Ho Shin} and Thorat, {Shivaji A.} and Hee Kim and Ha, {Hee Jin} and Kwanghyun Choi and Kim, {Young Ho} and Minseok Kim and Hwang, {Sun Wook} and Pearce, {Larry V.} and Esch, {Timothy E.} and Turcios, {Noe A.} and Blumberg, {Peter M.} and Jeewoo Lee",
note = "Funding Information: This research was supported by the Bio & Medical Technology Development Program of the National Research Foundation (NRF) funded by the Ministry of Science & ICT(NRF-2019R1A2C2006837), a grant of the Korea Health Technology R&D Project (Grant HI17C2325) through KHIDI funded by the Ministry of Health & Welfare, and the Intramural Research Program of the National Institutes of Health, Center for Cancer Research, National Cancer Institute (Project Z1A BC 005270). ",
year = "2020",
month = jan,
day = "9",
doi = "10.1021/acs.jmedchem.9b01046",
language = "English",
volume = "63",
pages = "418--424",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "1",
}