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Histamine, histamine receptors, and neuropathic pain relief

Lookup NU author(s): Dr Ilona Obara, Dr Seva TelezhkinORCiD, Ibrahim Alrashdi



This work is licensed under a Creative Commons Attribution 4.0 International License (CC BY 4.0).


Histamine, acting via distinct histamine H1 , H2 , H3 , and H4 receptors, 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 H3 receptor and H4 receptor in the modulation of neuropathic pain, which 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 presynaptic or postsynaptic neuronal membranes). 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.

Publication metadata

Author(s): Obara I, Telezhkin V, Alrashdi I, Chazot PL

Publication type: Article

Publication status: Published

Journal: British Journal of Pharmacology

Year: 2019

Volume: 177

Issue: 3

Pages: 580-599

Print publication date: 01/02/2020

Online publication date: 02/05/2019

Acceptance date: 18/04/2019

Date deposited: 19/09/2019

ISSN (print): 0007-1188

ISSN (electronic): 1476-5381

Publisher: John Wiley & Sons Ltd


DOI: 10.1111/bph.14696

PubMed id: 31046146


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