The vanilloid receptor TRPV1: 10 years from channel cloning to antagonist proof-of-concept.

1: Nat Rev Drug Discov. 2007 Apr 20; [Epub ahead of print]

Szallasi A, Cortright DN, Blum CA, Eid SR.

Department of Pathology, Monmouth Medical Center, Long Branch, New Jersey 07740 and Drexel University College of Medicine, Philadelphia, USA.

The clinical use of TRPV1 (transient receptor potential vanilloid subfamily, member 1; also known as VR1) antagonists is based on the concept that endogenous agonists acting on TRPV1 might provide a major contribution to certain pain conditions. Indeed, a number of small-molecule TRPV1 antagonists are already undergoing Phase I/II clinical trials for the indications of chronic inflammatory pain and migraine. Moreover, animal models suggest a therapeutic value for TRPV1 antagonists in the treatment of other types of pain, including pain from cancer. We argue that TRPV1 antagonists alone or in conjunction with other analgesics will improve the quality of life of people with migraine, chronic intractable pain secondary to cancer, AIDS or diabetes. Moreover, emerging data indicate that TRPV1 antagonists could also be useful in treating disorders other than pain, such as urinary urge incontinence, chronic cough and irritable bowel syndrome. The lack of effective drugs for treating many of these conditions highlights the need for further investigation into the therapeutic potential of TRPV1 antagonists.

PMID: 17464295 [PubMed – as supplied by publisher]

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Folllowing Rick Usher's death in December 2008, at his request in September of that year, I had agreed, as his principal contributor and an experienced journalist, to run the FMS Global News service due to his heavy commitments to music and raising research funds through this avenue. Following his sad and sudden death I hope to continue his work as he would have wished.
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