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Papers of the Week

Papers: 9 Nov 2019 - 15 Nov 2019

Animal Studies, Pharmacology/Drug Development

2020 Jan 09

J Med Chem



Discovery of Non-pungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic.


Ann J, Kim H S, Thorat SA, Kim H, Ha H, Choi K, Kim Y, Kim M S, Hwang S W, Pearce LV, Esch TE, Turcios NA, Blumberg PM, Lee J
J Med Chem. 2020 Jan 09; 63(1):418-424.
PMID: 31702924.


Paradoxically, some TRPV1 agonists are, at the organismal level, both non-pungent and clinically useful as topical analgesics. Here, we describe the scaled-up synthesis and characterization in mouse models of a novel, non-pungent vanilloid. Potent analgesic ac-tivity was observed in models of neuropathic pain, and the compound blocked capsaicin induced allodynia, showing dermal accu-mulation with little transdermal absorption. Finally, it displayed much weaker systemic toxicity compared to capsaicin and was negative in assays of genotoxicity.