Article
Identification of regions of the P2X(7) receptor that contribute to human and rat species differences in antagonist effects.
British journal of pharmacology - 1 Nov 2008
Michel A D, Clay W C, Ng S W, Roman S, Thompson K, Condreay J P, Hall M, Holbrook J, Livermore D, Senger S
Abstract excerpt
BACKGROUND AND PURPOSE: Several P2X(7) receptor antagonists are allosteric inhibitors and exhibit species difference in potency. Furthermore, N(2)-(3,4-difluorophenyl)-N(1)-(2-methyl-5-(1-piperazinylmethyl)phenyl)glycinamide dihydrochloride (GW791343) exhibits negative allosteric effects at the human P2X(7) receptor but is a positive allosteric modulator of the rat P2X(7) receptor. In this study we have...
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