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Pharmaceuticals (Basel). 2016 Aug 23;9(3). pii: E52. doi: 10.3390/ph9030052.

TRPV1: A Target for Rational Drug Design.

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Institute for Computational Molecular Science, Temple University, Philadelphia, PA 19122, USA.
New Jersey Medical School, Rutgers University, Newark, NJ 07103, USA.


Transient Receptor Potential Vanilloid 1 (TRPV1) is a non-selective, Ca(2+) 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.


TRPV1; capsaicin; nociception; pain; vanilloid

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