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Volume 375, Issue 1-2 p. 129-133
Research letter
Free Access

A P2X purinoceptor cDNA conferring a novel pharmacological profile

Xuenong Bo

Xuenong Bo

Department of Anatomy and Developmental Biology, University College London, Gower Street, London, WC 1E 6BT, UK

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Yi Zhang

Yi Zhang

Department of Anatomy and Developmental Biology, University College London, Gower Street, London, WC 1E 6BT, UK

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Mohammed Nassar

Mohammed Nassar

Wellcome Laboratory for Molecular Pharmacology and Department of Pharmacology, University College London, Gower Street, London WC 1E 6BT, UK

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Geoffrey Burnstock

Geoffrey Burnstock

Department of Anatomy and Developmental Biology, University College London, Gower Street, London, WC 1E 6BT, UK

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Ralf Schoepfer

Ralf Schoepfer

Wellcome Laboratory for Molecular Pharmacology and Department of Pharmacology, University College London, Gower Street, London WC 1E 6BT, UK

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First published: November 13, 1995
Citations: 219
Corresponding author. University College London, Department of Pharmacology, Gower Street, London, WC 1E 6BT, UK. Fax: (44) (171) 380 7245;

Abstract

We have cloned P2X4, a member of the P2-purinoceptor family, which has a new pharmacological profile. Rat P2X4 is distantly related to P2X1, P2X2 and P2X3 and is expressed in brain, spinal cord, lung, thymus, bladder, adrenal, testis and vas deferens. This ligand gated ion channel is activated by ATP and analogs with the potency order of ATP > ATPγS > 2-methylthio ATP > ADP ≈ αβ-methylene ATP. However, none of the currently used P2X purinoceptor antagonists suramin, reactive blue 2 and PPADS blocked ATP evoked currents; in contrast their application resulted in potentiation of the agonist response. Due to lack of any known antagonist for P2X4 it is unlikely that native P2X4 has previously been recognized as a P2X purinoceptor.