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 language | English |
|---|---|
| Pages (from-to) | 418-424 |
| Number of pages | 7 |
| Journal | Journal of Medicinal Chemistry |
| Volume | 63 |
| Issue number | 1 |
| DOIs | |
| Publication status | Published - 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