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

07:00 EST 8th November 2019 | BioPortfolio

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

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.

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This article was published in the following journal.

Name: Journal of medicinal chemistry
ISSN: 1520-4804
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Medical and Biotech [MESH] Definitions

A plant genus of the family SOLANACEAE. The hot peppers yield CAPSAICIN, which activates vanilloid receptors. Several varieties have sweet or pungent edible fruits that are used as vegetables when fresh and spices when the pods are dried.

A broad group of eukaryotic six-transmembrane cation channels that are classified by sequence homology because their functional involvement with SENSATION is varied. They have only weak voltage sensitivity and ion selectivity. They are named after a DROSOPHILA mutant that displayed transient receptor potentials in response to light. A 25-amino-acid motif containing a TRP box (EWKFAR) just C-terminal to S6 is found in TRPC, TRPV and TRPM subgroups. ANKYRIN repeats are found in TRPC, TRPV & TRPN subgroups. Some are functionally associated with TYROSINE KINASE or TYPE C PHOSPHOLIPASES.

The process of finding chemicals for potential therapeutic use.

The systematic search and discovery of natural substances which may have potential commercial applications.

A subgroup of TRP cation channels named after vanilloid receptor. They are very sensitive to TEMPERATURE and hot spicy food and CAPSAICIN. They have the TRP domain and ANKYRIN repeats. Selectivity for CALCIUM over SODIUM ranges from 3 to 100 fold.

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