Recent Patents on CNS Drug Discovery

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


TRPV1 Antagonists as a Potential Treatment for Hyperalgesia

Author(s): Louise A. Roberts and Mark Connor

Affiliation: Pain Management ResearchInstitute, Kolling Institute, Level 4, Main Block, University of Sydney atRoyal North Shore Hospital, E25. St. Leonards, NSW 2065, Sydney,Australia;


The vanilloid receptor (TRPV1) is a member of the transient receptor potential family of ion channels that is highly expressed in nociceptive primary afferent sensory neurons. TRPV1 is a voltage-dependent cation channel, which can be activated at physiological membrane potentials by stimuli including noxious heat ( > 42 degrees), capsaicin, hydrogen ions and anandamide. Activation of TRPV1 results in release of neurotransmitters from peripheral and central nerve terminals, resulting in pain and inflammation. Endogenous inflammatory mediators also promote activation of TRPV1. Studies in TRPV1 null mice reveal that responses to noxious heat stimuli are normal but the development of thermal hyperalgesia is abolished. Several TRPV1 antagonists have recently been developed and reported to alleviate or reverse mechanical and thermal hyperalgesia associated with inflammatory pain. This review will examine the development of patented TRPV1 antagonists as a potential clinical treatment for the alleviation of pain associated with hyperalgesia and inflammation.

Keywords: TRPV1, antagonist, hyperalgesia, capsaicin, sensory neuron, inflammation, pain

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Article Details

Page: [65 - 76]
Pages: 12
DOI: 10.2174/157488906775245309