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A “Cute” Desensitization of TRPV1

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Capsaicin and other vanilloids selectively excite and subsequently desensitize pain-conducting nerve fibers (nociceptors) and this process contributes to the analgesic (and thus therapeutically relevant) effects of these compounds. Such a desensitization process is triggered by the activation of the transient receptor potential vanilloid subtype 1 receptor channels (TRPV1) that open their cationic pores, permeable to sodium, potassium and calcium (Ca2+) ions. Depending on the duration of capsaicin exposure and the external calcium concentration, the Ca2+ influx via TRPV1 channels desensitizes the channels themselves, which, from the cellular point of view, represents a feedback mechanism protecting the nociceptive neuron from toxic Ca2+ overload. The ‘acute desensitization’ accounts for most of the reduction in responsiveness occurring within the first few (∼20) seconds after the vanilloids are administered to the cell for the first time. Another form of desensitization is ‘tachyphylaxis’, which is a reduction in the response to repeated applications of vanilloid. The wealth of pathways following TRPV1 activation that lead to increased intracellular Ca2+ levels and both forms of desensitization is huge and they might utilise just about every known type of signalling molecule. This review will not attempt to cover all historical aspects of research into all these processes. Instead, it will try to highlight some new challenging thoughts on the important phenomenon of TRPV1 desensitization and will focus on the putative mechanisms that are thought to account for the acute phase of this process.

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Keywords: A-kinase; ASIC receptor; Asp178; HEK293; Lys735; PIP2; Piperine; TRP channels; TRPV1 receptor; Tyr671; analgesia; anandamide; ankyrin-repeat domain; bradykinin; calmodulin; camphor; capsaicin; dephosphorylation; desensitization; diabetic neuropathy; mutagenesis studies; phorbol esters; phosphorylation; plethora; polymodal activation; postherpetic neuralgia; scaffolding protein; tachyphylaxis; transmembrane spanning

Document Type: Research Article

Publication date: 01 January 2011

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  • Current Pharmaceutical Biotechnology aims to cover all the latest and outstanding developments in Pharmaceutical Biotechnology. Each issue of the journal contains a series of timely in-depth reviews written by leaders in the field covering a range of current topics in both pre-clinical and clinical areas of Pharmaceutical Biotechnology. Current Pharmaceutical Biotechnology is an essential journal for academic, clinical, government and pharmaceutical scientists who wish to be kept informed and up-to-date with the latest and most important developments.
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