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Vol. 53, Issue 1, 107-118, March 2001

International Union of Pharmacology. XXIV. Current Status of the Nomenclature and Properties of P2X Receptors and Their Subunits

Baljit S. Khakh1, Geoffrey Burnstock, Charles Kennedy, Brian F. King, R. Alan North, Philippe Séguéla, Mark Voigt and Patrick P. A. Humphrey1

Division of Biology 156-29, California Institute of Technology, Pasadena, California (B.S.K.); Autonomic Neuroscience Institute, Royal Free Hospital School of Medicine, London, United Kingdom (G.B., B.F.K.); Department of Physiology and Pharmacology, University of Strathclyde, Royal College, Glasgow, United Kingdom (C.K.); Institute of Molecular Physiology, University of Sheffield, Western Bank, Sheffield, United Kingdom (R.A.N.); Department of Neurology and Neurosurgery, Montreal Neurological Institute, McGill University, Montreal, Quebec, Canada (P.S.); Pharmacological and Physiological Sciences, St. Louis University School of Medicine, St. Louis, Missouri (M.V.); and Glaxo Institute of Applied Pharmacology, University of Cambridge, Department of Pharmacology, Cambridge, United Kingdom (P.P.A.H.)

I. Introduction
II. Overall P2X Subunit Topology
III. Electrophysiological Properties of P2X Receptors
IV. Functional Properties of Homomeric Receptors
    A. P2X1
    B. P2X2
    C. P2X3
    D. P2X4
    E. P2X5
    F. P2X6
    G. P2X7
V. Functional Properties of Heteromeric Receptors
VI. Native Receptors in Whole Tissues
    A. Studies in Vitro
    B. Studies in Vivo
VII. Summary
Acknowledgments
References

ATP acts as a humoral mediator to control cell function extracellularly. The receptors that mediate the actions of ATP belong to two classes, the metabotropic P2Y receptors and the transmitter-gated, ion channel P2X receptors. This review describes the structure, distribution, function, and ligand recognition characteristics of P2X receptors, which comprise seven distinct subunits that can function as both homo- and hetero- polymers. The pharmacology of P2X receptors is complicated by marked differences between species orthologues. The current nomenclature is based largely on recombinant receptor studies and detailed knowledge of endogenous P2X receptors in native tissues is limited because of lack of good selective agonists and antagonists for each receptor type.

1 Address for correspondence: Baljit S. Khakh, Division of Neurobiology, MRC Laboratory of Molecular Biology, Hills Rd., Cambridge, CB2 2QH, UK. E-mail: bsk{at}mrc-lmb.cam.ac.uk or Patrick P. A. Humphrey, Glaxo Institute of Applied Pharmacology, University of Cambridge, Department of Pharmacology, Tennis Court Rd., Cambridge, CB2 1QJ UK. E-mail: ppah0562{at}glaxowellcome.co.uk

0031-6997/01/5301-0107$03.00/0
PHARMACOLOGICAL REVIEWS
Copyright © 2001 by The American Society for Pharmacology and Experimental Therapeutics


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