In this issue of Scandinavian Journal of Pain, Mayorga et al. report positive efficacy data of mavatrep, a transient receptor potential vanilloid subtype 1 (TRPV1) antagonist, in OA pain . A positive signal of efficacy has been reported previously in dental extraction pain , but this is the first report of a signal of efficacy with a TRPV1 antagonist in a chronic pain condition.1What is transient receptor potential vanilloid subtype 1 (TRPV1)?TRPV1 is a cation channel located on peripheral nociceptive fibres, but also in areas involved in nociception in the central nervous system [3,4]. The receptor is activated by heat, capsaicin and low pH and the activity is regulated by inflammatory regulators . The TRPV1 receptor acts as a polymodal signal detector and may be influenced by several simultaneous stimuli, e.g. the thermal activation curve for the TRPV1 receptor is shifted to the left by capsaicin .2Difficulties in developing this class of analgesic drugs – the TRPVl-anatagonistsBased on these properties, indicating a pivotal role for TRPV1 in nociception, many TRPV1 antagonists have been developed displaying efficacy in animal models of a variety of pain conditions, like inflammatory, osteoarthritis, and neuropathic pain models [5,7]. The clinical development of this class
Scandinavian Journal of Pain – de Gruyter
Published: Oct 1, 2017
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