1. The P2X4 Receptor: Cellular and Molecular Characteristics of a Promising Neuroinflammatory Target
- Author
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Reece Andrew Sophocleous, Lezanne Ooi, and Ronald Sluyter
- Subjects
P2X4 receptor ,P2RX4 gene ,purinergic receptor ,purinergic signalling ,extracellular ATP ,inflammation ,Biology (General) ,QH301-705.5 ,Chemistry ,QD1-999 - Abstract
The adenosine 5′-triphosphate-gated P2X4 receptor channel is a promising target in neuroinflammatory disorders, but the ability to effectively target these receptors in models of neuroinflammation has presented a constant challenge. As such, the exact role of P2X4 receptors and their cell signalling mechanisms in human physiology and pathophysiology still requires further elucidation. To this end, research into the molecular mechanisms of P2X4 receptor activation, modulation, and inhibition has continued to gain momentum in an attempt to further describe the role of P2X4 receptors in neuroinflammation and other disease settings. Here we provide an overview of the current understanding of the P2X4 receptor, including its expression and function in cells involved in neuroinflammatory signalling. We discuss the pharmacology of P2X4 receptors and provide an overview of P2X4-targeting molecules, including agonists, positive allosteric modulators, and antagonists. Finally, we discuss the use of P2X4 receptor modulators and antagonists in models of neuroinflammatory cell signalling and disease.
- Published
- 2022
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