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Review ArticleReview Article

Unravelling the Mystery of Capsaicin: A Tool to Understand and Treat Pain

Jessica O'Neill, Christina Brock, Anne Estrup Olesen, Trine Andresen, Matias Nilsson and Anthony H. Dickenson
Annette C. Dolphin, ASSOCIATE EDITOR
Pharmacological Reviews October 2012, 64 (4) 939-971; DOI: https://doi.org/10.1124/pr.112.006163
Jessica O'Neill
Neuroscience, Physiology and Pharmacology, University College London (J.O., A.H.D.); and Mech-Sense, Department of Gastroenterology, Aalborg Hospital, Aarhus University, Denmark (C.B., A.E.O., T.A., M.N.)
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Christina Brock
Neuroscience, Physiology and Pharmacology, University College London (J.O., A.H.D.); and Mech-Sense, Department of Gastroenterology, Aalborg Hospital, Aarhus University, Denmark (C.B., A.E.O., T.A., M.N.)
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Anne Estrup Olesen
Neuroscience, Physiology and Pharmacology, University College London (J.O., A.H.D.); and Mech-Sense, Department of Gastroenterology, Aalborg Hospital, Aarhus University, Denmark (C.B., A.E.O., T.A., M.N.)
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Trine Andresen
Neuroscience, Physiology and Pharmacology, University College London (J.O., A.H.D.); and Mech-Sense, Department of Gastroenterology, Aalborg Hospital, Aarhus University, Denmark (C.B., A.E.O., T.A., M.N.)
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Matias Nilsson
Neuroscience, Physiology and Pharmacology, University College London (J.O., A.H.D.); and Mech-Sense, Department of Gastroenterology, Aalborg Hospital, Aarhus University, Denmark (C.B., A.E.O., T.A., M.N.)
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Anthony H. Dickenson
Neuroscience, Physiology and Pharmacology, University College London (J.O., A.H.D.); and Mech-Sense, Department of Gastroenterology, Aalborg Hospital, Aarhus University, Denmark (C.B., A.E.O., T.A., M.N.)
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Annette C. Dolphin
Neuroscience, Physiology and Pharmacology, University College London (J.O., A.H.D.); and Mech-Sense, Department of Gastroenterology, Aalborg Hospital, Aarhus University, Denmark (C.B., A.E.O., T.A., M.N.)
Roles: ASSOCIATE EDITOR
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Abstract

A large number of pharmacological studies have used capsaicin as a tool to activate many physiological systems, with an emphasis on pain research but also including functions such as the cardiovascular system, the respiratory system, and the urinary tract. Understanding the actions of capsaicin led to the discovery its receptor, transient receptor potential (TRP) vanilloid subfamily member 1 (TRPV1), part of the superfamily of TRP receptors, sensing external events. This receptor is found on key fine sensory afferents, and so the use of capsaicin to selectively activate pain afferents has been exploited in animal studies, human psychophysics, and imaging studies. Its effects depend on the dose and route of administration and may include sensitization, desensitization, withdrawal of afferent nerve terminals, or even overt death of afferent fibers. The ability of capsaicin to generate central hypersensitivity has been valuable in understanding the consequences and mechanisms behind enhanced central processing of pain. In addition, capsaicin has been used as a therapeutic agent when applied topically, and antagonists of the TRPV1 receptor have been developed. Overall, the numerous uses for capsaicin are clear; hence, the rationale of this review is to bring together and discuss the different types of studies that exploit these actions to shed light upon capsaicin working both as a tool to understand pain but also as a treatment for chronic pain. This review will discuss the various actions of capsaicin and how it lends itself to these different purposes.

Footnotes

  • This article is available online at http://pharmrev.aspetjournals.org.

    http://dx.doi.org/10.1124/pr.112.006163.

  • © 2012 by The American Society for Pharmacology and Experimental Therapeutics
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Pharmacological Reviews: 64 (4)
Pharmacological Reviews
Vol. 64, Issue 4
1 Oct 2012
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Review ArticleReview Article

CAPSAICIN: TO UNDERSTAND AND TREAT PAIN

Jessica O'Neill, Christina Brock, Anne Estrup Olesen, Trine Andresen, Matias Nilsson and Anthony H. Dickenson
Pharmacological Reviews October 1, 2012, 64 (4) 939-971; DOI: https://doi.org/10.1124/pr.112.006163

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Review ArticleReview Article

CAPSAICIN: TO UNDERSTAND AND TREAT PAIN

Jessica O'Neill, Christina Brock, Anne Estrup Olesen, Trine Andresen, Matias Nilsson and Anthony H. Dickenson
Pharmacological Reviews October 1, 2012, 64 (4) 939-971; DOI: https://doi.org/10.1124/pr.112.006163
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  • Article
    • Abstract
    • I. Introduction
    • II. Physical and Chemical Properties of Capsaicin
    • III. Pharmacokinetics of Capsaicin
    • IV. Capsaicin Metabolism
    • V. Capsaicin Elimination
    • VI. Capsaicin Pharmacology
    • VII. Transient Receptor Potential Channels
    • VIII. Transient Receptor Potential Vanilloid 1
    • IX. Transient Receptor Potential Vanilloid 1 Splice Variants
    • X. Transient Receptor Potential Vanilloid 1 Polymorphisms
    • XI. Transient Receptor Potential Vanilloid 1 Receptor Expression in Humans in the Airways, Skin, and Viscera
    • XII. Experimental Pain Models
    • XIII. Sensitizing or Desensitizing?
    • XIV. Capsaicin As a Therapeutic Pharmacological Agent
    • XV. Conclusion
    • Acknowledgments
    • Authorship Contributions
    • Footnotes
    • References
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