Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic

Jihyae Ann, Ho Shin Kim, Shivaji A. Thorat, Hee Kim, Hee Jin Ha, Kwanghyun Choi, Young Ho Kim, Minseok Kim, Sun Wook Hwang, Larry V. Pearce, Timothy E. Esch, Noe A. Turcios, Peter M. Blumberg, Jeewoo Lee

Research output: Contribution to journalArticle

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.

Original languageEnglish
Pages (from-to)418-424
Number of pages7
JournalJournal of Medicinal Chemistry
Volume63
Issue number1
DOIs
Publication statusPublished - 2020 Jan 9

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Fingerprint Dive into the research topics of 'Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic'. Together they form a unique fingerprint.

  • Cite this

    Ann, J., Kim, H. S., Thorat, S. A., Kim, H., Ha, H. J., Choi, K., Kim, Y. H., Kim, M., Hwang, S. W., Pearce, L. V., Esch, T. E., Turcios, N. A., Blumberg, P. M., & Lee, J. (2020). Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic. Journal of Medicinal Chemistry, 63(1), 418-424. https://doi.org/10.1021/acs.jmedchem.9b01046