TRPV1: a therapeutic target for novel analgesic drugs?

The vanilloid receptor TRPV1 is now recognized as a molecular integrator of painful stimuli ranging from noxious heat to endovanilloids in inflammation. Pharmacological blockade of TRPV1 represents a new strategy in pain relief. TRPV1 antagonists are expected to prevent pain by silencing receptors w...

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Bibliographic Details
Published in:Trends in molecular medicine 2006-11, Vol.12 (11), p.545-554
Main Authors: Szallasi, Arpad, Cruz, Francisco, Geppetti, Pierangelo
Format: Article
Language:English
Subjects:
Analgesics - therapeutic use
Animals
Gene Targeting - methods
Humans
Inflammation - metabolism
Mice
Mice, Knockout
Migraine Disorders - metabolism
Models, Biological
Neurons, Afferent - metabolism
Pain - etiology
Pain - metabolism
Signal Transduction
Tissue Distribution
TRPV Cation Channels - antagonists & inhibitors
TRPV Cation Channels - genetics
TRPV Cation Channels - metabolism
TRPV Cation Channels - physiology
Urinary Bladder Diseases - metabolism
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Summary:The vanilloid receptor TRPV1 is now recognized as a molecular integrator of painful stimuli ranging from noxious heat to endovanilloids in inflammation. Pharmacological blockade of TRPV1 represents a new strategy in pain relief. TRPV1 antagonists are expected to prevent pain by silencing receptors where pain is generated rather than stopping the propagation of pain, as most-traditional pain killers do. This hypothesis has already being tested in the clinic by administering small molecule TRPV1 antagonists (e.g. GlaxoSmithKline SB-705498) for migraine and dental pain. Paradoxically, in some murine models of chronic pain, TRPV1-deficient mice exhibit more pain-related behavior than their wild-type littermates, indicating that the understanding of TRPV1 in pain is still incomplete. Moreover, there is mounting evidence to suggest the existence of functional TRPV1 both in the brain and in various non-neuronal tissues. The biological role of these receptors remains elusive, but their tissue distribution clearly indicates that they are involved in many more functions than just pain perception. Here, we review the potential therapeutic indications and adverse effects of TRPV1 antagonists.
ISSN:1471-4914
1471-499X
DOI:10.1016/j.molmed.2006.09.001