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Selectivity of diadenosine polyphosphates for rat P2X receptor subunits.

Wildman, Scott S.P., Brown, S G, King, B F, Burnstock, G (1999) Selectivity of diadenosine polyphosphates for rat P2X receptor subunits. European journal of pharmacology, 367 (1). pp. 119-23. ISSN 0014-2999. (doi:10.1016/S0014-2999(98)00976-5) (The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided)

The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided. (Contact us about this Publication)
Official URL
https://doi.org/10.1016/S0014-2999(98)00976-5

Abstract

The pharmacological activity of diadenosine polyphosphates was investigated at three recombinant P2X receptors (rat P2X1, rat P2X3, rat P2X4) expressed in Xenopus oocytes and studied under voltage-clamp conditions. For the rat P2X1 receptor, only P1,P6-diadenosine hexaphosphate (Ap6A) was a full agonist yet 2-3 folds less potent than ATP. At rat P2X3, P1,p4-diadenosine tetraphosphate (Ap4A), P1,P5-diadenosine pentaphosphate (Ap5A) and Ap6A were full agonists and more potent than ATP. Ap4A alone was equipotent with ATP at rat P2X4, but only as a partial agonist. Compared to known data for rat P2X2 and human P2X1 receptors, our findings contrast with rat P2X2 where only Ap4A is a full agonist although four folds less potent than ATP. At rat and human orthologues of P2X1, Ap5A was a partial agonist with similar potency. These data provide a useful basis for selective agonists of P2X receptor subunits.

Item Type: Article
DOI/Identification number: 10.1016/S0014-2999(98)00976-5
Uncontrolled keywords: Adenine dinucleotide; Diadenosine polyphosphate; P2X receptor; ATP; Xenopus oocyte
Subjects: R Medicine > RM Therapeutics. Pharmacology
Divisions: Faculties > Sciences > Medway School of Pharmacy
Depositing User: Scott S.P. Wildman
Date Deposited: 13 Dec 2015 13:51 UTC
Last Modified: 29 May 2019 16:40 UTC
Resource URI: https://kar.kent.ac.uk/id/eprint/52963 (The current URI for this page, for reference purposes)
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