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PMID: 7498461 Published · ppublish English Comparative Study Journal Article Research Support, Non-U.S. Gov't

A P2X purinoceptor cDNA conferring a novel pharmacological profile.

FEBS letters ·Vol. 375 ·No. 1-2 ·1995-11-13 ·Pages 129-33

Bo X, Zhang Y, Nassar M, Burnstock G, Schoepfer R

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 > ATP gamma S > 2-methylthio ATP > ADP approximately alpha beta-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.

MeSH Terms

Adenosine Triphosphate/analogs & derivatives,pharmacology Adrenal Glands/metabolism Amino Acid Sequence Animals Brain/metabolism Conserved Sequence Cysteine DNA, Complementary Female Hippocampus/metabolism In Situ Hybridization Ion Channel Gating Ion Channels/biosynthesis,drug effects,physiology Kinetics Lung/metabolism Male Membrane Potentials/drug effects Molecular Sequence Data Oocytes/drug effects,physiology Organ Specificity Rats Receptors, Purinergic P2/biosynthesis,drug effects,physiology Receptors, Purinergic P2X4 Sequence Homology, Amino Acid Spinal Cord/metabolism Suramin/pharmacology Testis/metabolism Thymus Gland/metabolism Vas Deferens/metabolism

Chemicals

DNA, Complementary Ion Channels P2rx4 protein, rat Receptors, Purinergic P2 Receptors, Purinergic P2X4 Suramin Adenosine Triphosphate Cysteine

Authors & Affiliations

5 authors, click to expand affiliations / ORCID

Bo X

Department of Anatomy and Developmental Biology, University College London, UK.

Zhang Y

Nassar M

Burnstock G

Schoepfer R

Article Info

Journal

FEBS letters

Abbr.

FEBS Lett

ISSN

0014-5793

DOI

10.1016/0014-5793(95)01203-q

Published

1995-11-13

Pages

129-33

Language

English

Region

England

NLM ID

0155157

Subset

Grants

Wellcome Trust · United Kingdom

Databases

GENBANK

X91200

External Links

PubMed source DOI: 10.1016/0014-5793(95)01203-q View journal details

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A P2X purinoceptor cDNA conferring a novel pharmacological profile.

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