Abstract
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.
Highlights
TRP ChannelsTransient Receptor Potential (TRP) channels were discovered while analyzing a visual mutant of drosophila that showed transient response to light, as opposed to the sustained receptor potential in wild type flies [1]
TRPV2 [13] is a capsaicin insensitive homolog of TRPV1, initially identified as a noxious heat sensor. It is activated with a heat threshold higher than that for TRPV1, and it is well expressed in peripheral sensory dorsal root ganglion (DRG) neurons [14]
TRPV1 was first described in small nociceptive DRG and trigeminal ganglion (TG) neurons
Summary
Transient Receptor Potential (TRP) channels were discovered while analyzing a visual mutant of drosophila that showed transient response to light, as opposed to the sustained receptor potential in wild type flies [1]. It is still unclear how this enzymatic cascade activates the channel responsible for generating the receptor potential in insects This channel complex includes dTRP protein, mutation of which was responsible for the transient light response [2]. Mutations in TRP channels cause human diseases as diverse as kidney disease (TRPC6), spontaneous pain syndrome (TRPA1), hypomagnesemia (TRPM6), night blindness (TRPM1) and complex musculoskeletal and neurological disorders (TRPV4) [6]. Given their widespread physiological roles and relatively recent discovery, many of them are promising drug targets [7]
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