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

Leanne Stokes; Janice A. Layhadi; Lucka Bibic; Kshitija Dhuna; Samuel J. Fountain

doi:10.3389/fphar.2017.00291

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

Leanne Stokes, Janice A. Layhadi, Lucka Bibic, Kshitija Dhuna, Samuel J. Fountain

Research output: Contribution to journal › Article › peer-review

107 Citations (Scopus)

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Abstract

ATP is a well-known extracellular signalling 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.

Original language	English
Article number	291
Journal	Frontiers in Pharmacology
Volume	8
DOIs	https://doi.org/10.3389/fphar.2017.00291
Publication status	Published - 23 May 2017

Keywords

ATP
P2X receptor
P2X4 receptor
Ivermectin
Microglial cells
Neuroinflammation
Pain
Pharmacology

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10.3389/fphar.2017.00291Licence: CC BY

fphar-08-00291Final published version, 778 KBLicence: CC BY

Samuel Fountain
- S.J.Fountainuea.acuk
- School of Biological Sciences - Professor of Pharmacology
- Cells and Tissues - Member
Person: Research Group Member, Academic, Teaching & Research
Leanne Stokes
- L.Stokesuea.acuk
- School of Chemistry, Pharmacy and Pharmacology - Associate Professor in Pharmacology
- Molecular and Tissue Pharmacology - Member
Person: Research Group Member, Academic, Teaching & Research

Enhancing microbial killing through the novel action of Panax ginseng derivatives on P2X7.
Stokes, L.
Biotechnology and Biological Sciences Research Council
26/09/16 → 25/09/19
Project: Research

Cite this

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title = "P2X4 receptor function in the nervous system and current breakthroughs in pharmacology",

abstract = "ATP is a well-known extracellular signalling 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.",

keywords = "ATP, P2X receptor, P2X4 receptor, Ivermectin, Microglial cells, Neuroinflammation, Pain, Pharmacology",

author = "Leanne Stokes and Layhadi, {Janice A.} and Lucka Bibic and Kshitija Dhuna and Fountain, {Samuel J.}",

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T1 - P2X4 receptor function in the nervous system and current breakthroughs in pharmacology

AU - Stokes, Leanne

AU - Layhadi, Janice A.

AU - Bibic, Lucka

AU - Dhuna, Kshitija

AU - Fountain, Samuel J.

PY - 2017/5/23

Y1 - 2017/5/23

N2 - ATP is a well-known extracellular signalling 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.

AB - ATP is a well-known extracellular signalling 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.

KW - ATP

KW - P2X receptor

KW - P2X4 receptor

KW - Ivermectin

KW - Microglial cells

KW - Neuroinflammation

KW - Pain

KW - Pharmacology

U2 - 10.3389/fphar.2017.00291

DO - 10.3389/fphar.2017.00291

M3 - Article

VL - 8

JO - Frontiers in Pharmacology

JF - Frontiers in Pharmacology

SN - 1663-9812

M1 - 291

ER -

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

Abstract

Keywords

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Profiles

Samuel Fountain

Leanne Stokes

Projects

Enhancing microbial killing through the novel action of Panax ginseng derivatives on P2X7.

Cite this