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Histamine, histamine receptors and neuropathic pain relief

Obara, Ilona; Telezhkin, Vsevolod; Alrashdi, Ibrahim; Chazot, Paul L.

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Ilona Obara

Vsevolod Telezhkin

Ibrahim Alrashdi


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.


Obara, I., Telezhkin, V., Alrashdi, I., & Chazot, P. L. (2020). Histamine, histamine receptors and neuropathic pain relief. British Journal of Pharmacology, 177(3), 580-599.

Journal Article Type Article
Acceptance Date Apr 18, 2019
Online Publication Date Jun 7, 2019
Publication Date Feb 28, 2020
Deposit Date May 3, 2019
Publicly Available Date Jun 12, 2019
Journal British Journal of Pharmacology
Print ISSN 0007-1188
Electronic ISSN 1476-5381
Publisher Wiley
Peer Reviewed Peer Reviewed
Volume 177
Issue 3
Pages 580-599


Published Journal Article (Advance online version) (1.1 Mb)

Copyright Statement
Advance online version © 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.

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