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Pharmaceuticals 2016, 9(3), 52;

TRPV1: A Target for Rational Drug Design

Institute for Computational Molecular Science, Temple University, Philadelphia, PA 19122, USA
New Jersey Medical School, Rutgers University, Newark, NJ 07103, USA
Authors to whom correspondence should be addressed.
Academic Editors: Arpad Szallasi and Susan M. Huang
Received: 13 July 2016 / Revised: 12 August 2016 / Accepted: 18 August 2016 / Published: 23 August 2016
Full-Text   |   PDF [1308 KB, uploaded 23 August 2016]   |  


Transient Receptor Potential Vanilloid 1 (TRPV1) is a non-selective, Ca2+ permeable cation channel activated by noxious heat, and chemical ligands, such as capsaicin and resiniferatoxin (RTX). Many compounds have been developed that either activate or inhibit TRPV1, but none of them are in routine clinical practice. This review will discuss the rationale for antagonists and agonists of TRPV1 for pain relief and other conditions, and strategies to develop new, better drugs to target this ion channel, using the newly available high-resolution structures. View Full-Text
Keywords: TRPV1; capsaicin; vanilloid; pain; nociception TRPV1; capsaicin; vanilloid; pain; nociception

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Carnevale, V.; Rohacs, T. TRPV1: A Target for Rational Drug Design. Pharmaceuticals 2016, 9, 52.

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