P2X4 receptor function in the nervous system and current breakthroughs in pharmacology

Stokes, L, Layhadi, J, Bibic, L, Dhuna, K and Fountain, S 2017, 'P2X4 receptor function in the nervous system and current breakthroughs in pharmacology', Frontiers in Pharmacology, vol. 8, 291, pp. 1-15.


Document type: Journal Article
Collection: Journal Articles

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Title P2X4 receptor function in the nervous system and current breakthroughs in pharmacology
Author(s) Stokes, L
Layhadi, J
Bibic, L
Dhuna, K
Fountain, S
Year 2017
Journal name Frontiers in Pharmacology
Volume number 8
Article Number 291
Start page 1
End page 15
Total pages 15
Publisher Frontiers Research Foundation
Abstract Adenosine 5'-triphosphate is a well-known extracellular signaling molecule and neurotransmitter known to activate purinergic P2X receptors. Information has been elucidated about the structure and gating of P2X channels following the determination of the crystal structure of P2X4 (zebrafish), however, there is still much to discover regarding the role of this receptor in the central nervous system (CNS). In this review we provide an overview of what is known about P2X4 expression in the CNS and discuss evidence for pathophysiological roles in neuroinflammation and neuropathic pain. Recent advances in the development of pharmacological tools including selective antagonists (5-BDBD, PSB-12062, BX430) and positive modulators (ivermectin, avermectins, divalent cations) of P2X4 will be discussed.
Subject Pharmacology and Pharmaceutical Sciences not elsewhere classified
Keyword(s) Antagonist
ATP
Ivermectin
Microglia
P2X4
Pain
DOI - identifier 10.3389/fphar.2017.00291
Copyright notice Copyright © 2017 Stokes, Layhadi, Bibic, Dhuna and Fountain. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
ISSN 1663-9812
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