TRPV1: a therapeutic target for novel analgesic drugs?

• Type: Another Publication in an International Scientific Journal
• Date: 2006

Authors

Szallasi, A (Author) Other; Francisco Cruz (Author) FMUP; Geppetti, P (Author) Other

Journal

Title: Trends in Molecular Medicine

Vol. 12

Pages: 545-554

ISSN: 1471-4914

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 145 Citations

Scopus - 167 Citations

Other information

Authenticus ID: P-004-GGC

DOI: 10.1016/j.molmed.2006.09.001

Abstract (EN): 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. GlaxoSmithKIine SB705498) for migraine and dental pain. Paradoxically, in some murine models of chronic pain, TRPV1-deficient mice exhibit more pain-related behavior than their wildtype 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.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 10