P2X receptors and nociception

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P2X receptors and nociception.

The potential importance for nociception of P2X receptors, the ionotropic receptors activated by ATP, is underscored by the variety of pain states in which this endogenous ligand can be released. Several important findings have been made recently indicating that P2X receptors can be involved in pain mechanisms both centrally and in the periphery. The roles of ATP at these two sites and the P2X ...

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P2X receptors.

Extracellular adenosine 5'-triphosphate (ATP) activates cell surface P2X and P2Y receptors. P2X receptors are membrane ion channels preferably permeable to sodium, potassium and calcium that open within milliseconds of the binding of ATP. In molecular architecture, they form a unique structural family. The receptor is a trimer, the binding of ATP between subunits causes them to flex together wi...

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P2X and P2Y Receptors

Kenneth Jacobson serves as Chief of the Laboratory of Bioorganic Chemistry and the Molecular Recognition Section at the National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health in Bethesda, Maryland, USA. Dr. Jacobson is a medicinal chemist with interests in the structure and pharmacology of G-proteincoupled receptors, in particular receptors for adenosine...

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Subunit arrangement in P2X receptors.

ATP-gated ionotropic receptors (P2X receptors) are distributed widely in the nervous system. For example, a hetero-oligomeric receptor containing both P2X2 and P2X3 subunits is involved in primary afferent sensation. Each subunit has two membrane-spanning domains. We have used disulfide bond formation between engineered cysteines to demonstrate close proximity between the outer ends of the firs...

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Signaling at purinergic P2X receptors.

P2X receptors are membrane cation channels gated by extracellular ATP. Seven P2X receptor subunits (P2X(1-7)) are widely distributed in excitable and nonexcitable cells of vertebrates. They play key roles in inter alia afferent signaling (including pain), regulation of renal blood flow, vascular endothelium, and inflammatory responses. We summarize the evidence for these and other roles, emphas...

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ژورنال

عنوان ژورنال: Japanese Journal of Pharmacology

سال: 2000

ISSN: 0021-5198

DOI: 10.1016/s0021-5198(19)47612-9