Abstract
Decades of characterization of the transient receptor potential vanilloid subtype 1 (TRPV1) has led to the realization of its central role in thermosensation and pain perception. A large number of pharmaceutical companies have had interest in developing TPRV1 antagonists for the treatment of pain. The subsequent discovery of multiple other members of this TRPV family has not gone unnoticed. TRPV3 exhibits approximately 40% homology to TRPV1, and has common as well as distinct features from TRPV1 in channel physiology, expression and function. Here we review the current understanding of TRPV3 channel biology, activation, sensitization and the consequences of TRPV3 manipulation for thermosensation and nociception, as well as additional considerations regarding the expression of TRPV3 in the skin. We weigh in on the available evidence in the context of potential development of TRPV3 modulating agents as analgesics.
Highlights
Transient receptor potential vanilloid subtype 3 (TRPV3) is a member of the TRP vanilloid subtype family
TRPV3 was the first receptor identified in the TRP channel family that is activated by warm temperatures
TRPV3 is reported to be activated by multiple different chemical agonists. 2-Aminoethyl diphenylborinate (2-APB) and its structural analog diphenylboronic anhydride (DPBA) activate TRPV3 efficaciously [17, 22, 23]
Summary
Transient receptor potential vanilloid subtype 3 (TRPV3) is a member of the TRP vanilloid subtype family. TRPV3 is reported to be activated by multiple different chemical agonists. Further analysis of functional structures would facilitate the development of therapeutics targeting agonist- or pathology-specific activation of TRPV3.
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