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Histamine, histamine receptors and neuropathic pain relief.

Obara, Ilona and Telezhkin, Vsevolod and Alrashdi, Ibrahim and Chazot, Paul L. (2020) 'Histamine, histamine receptors and neuropathic pain relief.', British journal of pharmacology., 177 (3). pp. 580-599.


Histamine, acting via distinct histamine H1, H2, H3 and H4 receptors (H1R, H2R, H3R, H4R), regulates various physiological and pathological processes, including pain. In the last two decades, there has been a particular increase in evidence to support the involvement of H3R and H4R in the modulation of neuropathic pain, that remains challenging in terms of management. However, recent data show contrasting effects on neuropathic pain due to multiple factors that determine the pharmacological responses of histamine receptors and their underlying signal transduction properties (e.g., localization on either the pre‐ or postsynaptic neuronal membrane). This review summarizes the most recent findings on the role of histamine and the effects mediated by the four histamine receptors in response to the various stimuli associated with and promoting neuropathic pain. We particularly focus on mechanisms underlying histamine‐mediated analgesia, as we aim to clarify the analgesic potential of histamine receptor ligands in neuropathic pain.

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Publisher statement:© 2019 The Authors. British Journal of Pharmacology published by John Wiley & Sons Ltd on behalf of British Pharmacological Society. This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
Date accepted:18 April 2019
Date deposited:03 May 2019
Date of first online publication:07 June 2019
Date first made open access:13 February 2020

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