Selectivity of diadenosine polyphosphates for rat P2X receptor subunits

Wildman, Scott, Brown, Sean G, King, Brian F and Burnstock, Geoffrey (1999) Selectivity of diadenosine polyphosphates for rat P2X receptor subunits. European Journal of Pharmacology, 367. pp. 119-123. ISSN 00142999

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.

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Official URL:	https://doi.org/10.1016/s0014-2999(98)00976-5
Item Type:	Article
Depositing User:	Saxony Anders
Date Deposited:	12 Jul 2023 09:22
Last Modified:	13 Nov 2024 13:55
URI:	https://nul.repository.guildhe.ac.uk/id/eprint/97

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