Journal
EXPERT OPINION ON INVESTIGATIONAL DRUGS
Volume 13, Issue 11, Pages 1445-1456Publisher
ASHLEY PUBLICATIONS LTD
DOI: 10.1517/13543784.13.11.1445
Keywords
analgesia; bladder; capsaicin; joints; nociceptors; pain; skin; TRPV1
Categories
Ask authors/readers for more resources
Capsaicin and other naturally occurring pungent molecules have been used for centuries as topical analgesics and rubefactants to treat a variety of chronically painful conditions. Recently, instillations of high-concentration capsaicin and resiniferatoxin solutions have been found to be useful for the management of persistent bladder pain or overactive bladder. However, only within the last 7 years has it been appreciated that the selective action of these compounds on a subset of sensory nerve fibres is mediated by agonist activity at a ligand-gated ion channel called the transient receptor potential vanilloid receptor 1 (TRPV1). Accordingly, this discovery has fueled intensive research and drug development efforts, mainly in a search for novel analgesic or anti-inflammatory therapies. Two different but non-mutually exclusive, strategies are being pursued: optimisation of TRPV1 agonist-based therapies, which can functionally inactivate nociceptive nerve fibres, and identification of receptor antagonists, which would prevent nociceptive fibres from being activated by ongoing inflammatory stimuli. Available information on TRPV1 agonists; in development and their biological rationale will be summarised in this review.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available