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      Capsaicin: Current Understanding of Its Mechanisms and Therapy of Pain and Other Pre-Clinical and Clinical Uses

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          Abstract

          In this review, we discuss the importance of capsaicin to the current understanding of neuronal modulation of pain and explore the mechanisms of capsaicin-induced pain. We will focus on the analgesic effects of capsaicin and its clinical applicability in treating pain. Furthermore, we will draw attention to the rationale for other clinical therapeutic uses and implications of capsaicin in diseases such as obesity, diabetes, cardiovascular conditions, cancer, airway diseases, itch, gastric, and urological disorders.

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          Most cited references259

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          Impaired nociception and pain sensation in mice lacking the capsaicin receptor.

          The capsaicin (vanilloid) receptor VR1 is a cation channel expressed by primary sensory neurons of the "pain" pathway. Heterologously expressed VR1 can be activated by vanilloid compounds, protons, or heat (>43 degrees C), but whether this channel contributes to chemical or thermal sensitivity in vivo is not known. Here, we demonstrate that sensory neurons from mice lacking VR1 are severely deficient in their responses to each of these noxious stimuli. VR1-/- mice showed normal responses to noxious mechanical stimuli but exhibited no vanilloid-evoked pain behavior, were impaired in the detection of painful heat, and showed little thermal hypersensitivity in the setting of inflammation. Thus, VR1 is essential for selective modalities of pain sensation and for tissue injury-induced thermal hyperalgesia.
            • Record: found
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            • Article: not found

            Neurogenic inflammation and the peripheral nervous system in host defense and immunopathology.

            The peripheral nervous and immune systems are traditionally thought of as serving separate functions. The line between them is, however, becoming increasingly blurred by new insights into neurogenic inflammation. Nociceptor neurons possess many of the same molecular recognition pathways for danger as immune cells, and, in response to danger, the peripheral nervous system directly communicates with the immune system, forming an integrated protective mechanism. The dense innervation network of sensory and autonomic fibers in peripheral tissues and high speed of neural transduction allows rapid local and systemic neurogenic modulation of immunity. Peripheral neurons also seem to contribute to immune dysfunction in autoimmune and allergic diseases. Therefore, understanding the coordinated interaction of peripheral neurons with immune cells may advance therapeutic approaches to increase host defense and suppress immunopathology.
              • Record: found
              • Abstract: not found
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              Vanilloid (Capsaicin) receptors and mechanisms.

                Author and article information

                Contributors
                Role: Academic Editor
                Journal
                Molecules
                Molecules
                molecules
                Molecules
                MDPI
                1420-3049
                28 June 2016
                July 2016
                : 21
                : 7
                : 844
                Affiliations
                Departamento de Ciências Patológicas, Centro de Ciências Biológicas, Universidade Estadual de Londrina, Rodovia Celso Garcia Cid KM480 PR445, Caixa Postal 10.011, 86057-970 Londrina, Paraná, Brazil; vfattori@ 123456outlook.com (V.F.); hohmann.miriam@ 123456gmail.com (M.S.N.H.); anacrossaneis@ 123456gmail.com (A.C.R.); pinho.fe@ 123456gmail.com (F.A.P.-R.)
                Author notes
                [* ]Correspondence: waverri@ 123456uel.br or waldiceujr@ 123456yahoo.com.br ; Tel.: +55-43-3371-4979
                [†]

                These authors contributed equally to this paper.

                Article
                molecules-21-00844
                10.3390/molecules21070844
                6273101
                27367653
                9949d5de-6e55-4f45-9c7e-e73600247a37
                © 2016 by the authors.

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license ( http://creativecommons.org/licenses/by/4.0/).

                History
                : 27 April 2016
                : 27 April 2016
                Categories
                Review

                analgesia,capsaicinoids,chili peppers,desensitization,trpv1
                analgesia, capsaicinoids, chili peppers, desensitization, trpv1

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