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Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic
- Authors
- Ann, Jihyae; Kim, Ho Shin; Thorat, Shivaji A.; Kim, Hee; Ha, Hee-Jin; Choi, Kwanghyun; Kim, Young-Ho; Kim, Minseok; Hwang, Sun Wook; Pearce, Larry, V; Esch, Timothy E.; Turcios, Noe A.; Blumberg, Peter M.; Lee, Jeewoo
- Issue Date
- Jan-2020
- Publisher
- American Chemical Society
- Citation
- Journal of Medicinal Chemistry, v.63, no.1, pp 418 - 424
- Pages
- 7
- Indexed
- SCIE
SCOPUS
- Journal Title
- Journal of Medicinal Chemistry
- Volume
- 63
- Number
- 1
- Start Page
- 418
- End Page
- 424
- ISSN
- 0022-2623
1520-4804
- 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.
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Collections - 3. Graduate School > Biomedical Research Center > 1. Journal Articles
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Related Researcher
- Hwang, Sun Wook
- College of Medicine (Department of Convergence Medicine)