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TRPV3 in Drug Development

Use of Capsaicin to Treat Pain: Mechanistic and Therapeutic Considerations

Department of Neural and Pain Sciences, University of Maryland, School of Dentistry, Program in Neuroscience, Center to Advance Chronic Pain Research, Baltimore, MD 21201, USA
Centrexion Therapeutics, Baltimore, MD 21202, USA
Authors to whom correspondence should be addressed.
Academic Editors: Arpad Szallasi and Susan M. Huang
Pharmaceuticals 2016, 9(4), 66;
Received: 7 September 2016 / Revised: 25 October 2016 / Accepted: 27 October 2016 / Published: 1 November 2016
Capsaicin is the pungent ingredient of chili peppers and is approved as a topical treatment of neuropathic pain. The analgesia lasts for several months after a single treatment. Capsaicin selectively activates TRPV1, a Ca2+-permeable cationic ion channel that is enriched in the terminals of certain nociceptors. Activation is followed by a prolonged decreased response to noxious stimuli. Interest also exists in the use of injectable capsaicin as a treatment for focal pain conditions, such as arthritis and other musculoskeletal conditions. Recently injection of capsaicin showed therapeutic efficacy in patients with Morton’s neuroma, a painful foot condition associated with compression of one of the digital nerves. The relief of pain was associated with no change in tactile sensibility. Though injection evokes short term pain, the brief systemic exposure and potential to establish long term analgesia without other sensory changes creates an attractive clinical profile. Short-term and long-term effects arise from both functional and structural changes in nociceptive terminals. In this review, we discuss how local administration of capsaicin may induce ablation of nociceptive terminals and the clinical implications. View Full-Text
Keywords: capsaicin; pain; nociceptors; TRPV1 receptors capsaicin; pain; nociceptors; TRPV1 receptors
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MDPI and ACS Style

Chung, M.-K.; Campbell, J.N. Use of Capsaicin to Treat Pain: Mechanistic and Therapeutic Considerations. Pharmaceuticals 2016, 9, 66.

AMA Style

Chung M-K, Campbell JN. Use of Capsaicin to Treat Pain: Mechanistic and Therapeutic Considerations. Pharmaceuticals. 2016; 9(4):66.

Chicago/Turabian Style

Chung, Man-Kyo, and James N. Campbell. 2016. "Use of Capsaicin to Treat Pain: Mechanistic and Therapeutic Considerations" Pharmaceuticals 9, no. 4: 66.

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