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Molecular cloning and characterization of rat P2Y4 nucleotide receptor.

Bogdanov, Y. D., Wildman, Scott S.P., Clements, M. P., King, Brian F., Burnstock, Geoffrey (1998) Molecular cloning and characterization of rat P2Y4 nucleotide receptor. British Journal of Pharmacology, 124 (3). pp. 428-430. ISSN 0007-1188. E-ISSN 1476-5381. (doi:10.1038/sj.bjp.0701880) (Access to this publication is currently restricted. You may be able to access a copy if URLs are provided)

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Abstract

An intronless open reading frame encoding a protein (361aa in length) was isolated from a rat genomic library probed with a DNA fragment from rat heart. This protein showed 83% sequence identity with the human P2Y4 (hP2Y4) receptor and represents a homologue of the human pyrimidinoceptor. However, the rP2Y4 receptor is not selective for uridine nucleotides and, instead, shows an agonist potency order of ITP = ATP = ADP(pure) = UTP = ATPgammaS = 2-MeSATP = Ap4A > UDP(pure). ADP, ATPgammaS, 2-MeSATP and UDP are partial agonists. Thus, in terms of agonist profile, rP2Y4 is more like the P2U receptor subtype. The rP2Y4 receptor was reversibly antagonized by Reactive blue 2 but not by suramin which, otherwise, inhibits the hP2Y2 receptor (a known P2U receptor). Thus, rP2Y4 and the P2Y2 subtype appear to be structurally distinct forms of the P2U receptor (where ATP and UTP are equi-active) but can be distinguished as suramin-insensitive and suramin-sensitive P2U receptors, respectively.

Item Type: Article
DOI/Identification number: 10.1038/sj.bjp.0701880
Uncontrolled keywords: P2Y4 receptor; nucleotide receptor; pyrimidinoceptor; P2U receptor; ATP; UTP; Xenopus oocytes
Subjects: Q Science
R Medicine > RM Therapeutics. Pharmacology
Divisions: Faculties > Sciences > Medway School of Pharmacy
Depositing User: Scott S.P. Wildman
Date Deposited: 09 Dec 2015 14:35 UTC
Last Modified: 29 May 2019 16:40 UTC
Resource URI: https://kar.kent.ac.uk/id/eprint/52954 (The current URI for this page, for reference purposes)
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