GW791343 HCl - CAS 309712-55-8
Catalog number: 309712-55-8
Category: Inhibitor
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P2X Receptor
GW791343 HCl is aHCl salt form of GW791343, which is a non-competitive allosteric modulator of human P2X7 receptor inhibitor with pIC50 of 7.
GW791343; GW 791343; GW-791343; 1019779-04-4;
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1.Identification of regions of the P2X(7) receptor that contribute to human and rat species differences in antagonist effects.
Michel AD;Clay WC;Ng SW;Roman S;Thompson K;Condreay JP;Hall M;Holbrook J;Livermore D;Senger S Br J Pharmacol. 2008 Nov;155(5):738-51. doi: 10.1038/bjp.2008.306. Epub 2008 Jul 28.
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 identified several regions of the P2X(7) receptor that contribute to the species differences in antagonist effects.;EXPERIMENTAL APPROACH: ;Chimeric human-rat P2X(7) receptors were constructed with regions of the rat receptor being inserted into the human receptor. Antagonist effects at these receptors were measured in ethidium accumulation and radioligand binding studies.;KEY RESULTS: ;Exchanging regions of the P2X(7) receptor close to transmembrane domain 1 modified the effects of KN62, 4-(4-fluorophenyl)-2-(4-methylsulphinylphenyl)-5-(4-pyridyl)1H-imidazole (SB203580) and GW791343. Further studies, in which single amino acids were exchanged, identified amino acid 95 as being primarily responsible for the differential allosteric effects of GW791343 and, to varying degrees, the species differences in potency of SB203580 and KN62.
2.Negative and positive allosteric modulators of the P2X(7) receptor.
Michel AD;Chambers LJ;Walter DS Br J Pharmacol. 2008 Feb;153(4):737-50. Epub 2007 Dec 10.
BACKGROUND AND PURPOSE: ;Antagonist effects at the P2X(7) receptor are complex with many behaving in a non-competitive manner. In this study, the effects of N-[2-({2-[(2-hydroxyethyl)amino]ethyl}amino)-5-quinolinyl]-2-tricyclo[,7)]dec-1-ylacetamide (compound-17) and N (2)-(3,4-difluorophenyl)-N (1)-[2-methyl-5-(1-piperazinylmethyl)phenyl]glycinamide dihydrochloride (GW791343) on P2X(7) receptors were examined and their mechanism of action explored.;EXPERIMENTAL APPROACH: ;Antagonist effects were studied by measuring agonist-stimulated ethidium accumulation in cells expressing human or rat recombinant P2X(7) receptors and in radioligand binding studies.;KEY RESULTS: ;Compound-17 and GW791343 were non-competitive inhibitors of human P2X(7) receptors. Receptor protection studies using decavanadate and pyridoxalphosphate-6-azophenyl-2',4'-disulphonic acid (PPADS) showed that neither compound-17 nor GW791343 competitively interacted at the ATP binding site and so were probably negative allosteric modulators of the P2X(7) receptor. GW791343 prevented the slowly reversible blockade of the human P2X(7) receptor produced by compound-17 and inhibited [(3)H]-compound-17 binding to the P2X(7) receptor suggesting they may bind to similar or interacting sites.
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CAS 309712-55-8 GW791343 HCl

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