GW 791343 hydrochloride Inhibitor CAS No. 309712-55-8

Product Name	GW 791343 hydrochloride
CAS No.	309712-55-8
Molecular Weight	483.81
Formula	C₂₀H₂₇Cl₃F₂N₄O
Chemical Name	2-[(3,4-Difluorophenyl)amino]-N-[2-methyl-5-(1-piperazinylmethyl)phenyl]acetamide hydrochloride
Smiles	C(=O)(CNc1cc(c(cc1)F)F)Nc1c(ccc(c1)CN1CCNCC1)C Cl Cl Cl
Chemical Structure

Biological activities

GW 791343 hydrochloride is a hydrochloride salt form of GW791343 which is a positive allosteric modulator of the rat P2X7 receptor. In cells expressing human P2X7 receptors, GW 791343 inhibits agonist-stimulated ethidium accumulation in both sucrose and NaCl buffer, although the effects differ slightly between the buffers. In NaCl buffer, GW 791343 reduces the maximal response to both ATP and BzATP, but there is little effect on agonist potency except for a decrease in the presence of 300??000 nM GW 791343. GW791343 also reduces maximal responses to ATP and BzATP in sucrose buffer, although this effect is more marked when using ATP as agonist. In sucrose buffer, GW791343 produces a slight decrease in ATP potency at 300 nM and decreases BzATP potency at concentrations of 300 nM to 10 µM. GW 791343 does not interact at the same site as PPADS (pyridoxalphosphate-6-azophenyl-2??4??disulphonic acid) or decavanadate, which is presumed to be the ATP binding site, and so GW 791343 appears to be a negative allosteric modulator of the human P2X7 receptor. ^[1] GW791343 inhibits responses at the human??at chimeric receptor in both sucrose and NaCl buffer. GW791343 increases responses to BzATP at the F95L mutant receptor. ^[2]

References

[1] Michel AD, et al. Br J Pharmacol. Negative and positive allosteric modulators of the P2X(7) receptor. 2008, 153(4): 737-750. [2] Michel AD, et al. Identification of regions of the P2X(7) receptor that contribute to human and rat species differences in antagonist effects. Br J Pharmacol. 2008, 155(5): 738-751.

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