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P2X4 Receptor Function in the Nervous System and Current Breakthroughs in Pharmacology

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

Front Pharmacol. 2017 May 23;8:291.

PMID: 28588493

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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP55476476 PSB-12062 PSB-12062 55476-47-6 Price
AP688309708 BX430 BX430 688309-70-8 Price
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