Modulation of the TRPV1 Channel: Current Clinical Trials and Recent Patents with Focus on Neurological Conditions

ISSN: 2212-3954 (Online)
ISSN: 1574-8898 (Print)


Volume 9, 3 Issues, 2014


Download PDF Flyer




Recent Patents on CNS Drug Discovery

Aims & ScopeAbstracted/Indexed in


Submit Abstracts Online Submit Manuscripts Online

Editor-in-Chief:
Vincenzo Di Marzo
Istituto di Chimica Biomolecolare (I.C.B.)
Consiglio Nazionale delle Ricerche (C.N.R.)
Via Campi Flegrei 34
Pozzuoli, Napoli 80078
Italy


View Full Editorial Board

Subscribe Purchase Articles Order Reprints


Modulation of the TRPV1 Channel: Current Clinical Trials and Recent Patents with Focus on Neurological Conditions

Author(s): Luciano De Petrocellis and Aniello S. Moriello

Affiliation: Endocannabinoid Research Group, Institute of Biomolecular Chemistry, CNR, Pozzuoli, Italy.

Abstract

The transient receptor potential vanilloid-1 cat ion channel (TRPV1) is a nonspecific cation channel that can be activated by multiple endogenous stimuli and is expressed predominantly in sensory neurons, where it serves as a key nodal point in pain transmission pathways. In mammals, TRPV1 displays a wide tissue and cellular expression including both the peripheral and central nervous system, and in the latter it is now recognized to have a broader distribution and function. The pharmacological modulation of TRPV1 represents a strategy for the treatment of a variety of disease states, particularly those requiring chronic pain management. The validation of the TRPV1 channel as a therapeutic target for the control of pain and inflammatory conditions in a variety of diseases and injury states, has prompted the development of several TRPV1 agonists and antagonists that have entered clinical trials. Studies comparing the analgesic effects of TRPV1 antagonists with and without significant CNS penetration demonstrated that a dual (both peripheral and central) action is required to produce broad-spectrum analgesia. TRPV1 can be considered as a target for next generation analgesics. However, although a number of compounds are in clinical trials, the therapeutic utility of TRPV1 agonist and antagonists is yet to be validated unequivocally. This review summarizes current clinical trials and recent patents with small molecule TRPV1 agonists and antagonists with a focus on neurological conditions.

Keywords: Inflammation, pain, TRPV1.

Purchase Online Order Reprints Order Eprints Rights and Permissions

  
  



Article Details

Volume: 8
Issue Number: 3
First Page: 180
Last Page: 204
Page Count: 25
DOI: 10.2174/1574889808666131209124012
Advertisement

Related Journals




Webmaster Contact: urooj@benthamscience.org Copyright © 2014 Bentham Science