GW791343 hydrochloride is a non-competitive human P2X (7) receptor inhibitor with pIC50 of about 7.1. GW791343 hydrochloride exhibits negative allosteric effects at the human P2X (7) receptor but is a positive allosteric modulator of the rat P2X (7) receptor. GW791343 hydrochloride competitively interacted at the ATP binding site and so were probably negative allosteric modulators of the P2X (7) receptor. GW791343 hydrochloride increased responses to BzATP at the F95L mutant receptor, although the magnitude of this effect was not as marked as at the rat ECD, rat–human or domain 1 receptor.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Related P2 Receptor Products|
|Suramin sodium salt
Suramin sodium salt is a polysulfonated naphthylurea that inhibits the binding of calmodulin to recognition sites on the ryanodine receptor-1 (IC50 = 4.9 μM), blocks G protein coupling to GPCRs, and non-selectively antagonizes P2 purinergic receptors (10-100 μM).
|Clopidogrel hydrogen sulfate
S-(+)-Clopidogrel Hydrogen Sulfate is the S enantiomer of clopidogrel and a P2Y12 receptor inhibitor.
Clopidogrel (Plavix) is an oral, thienopyridine class antiplatelet agent used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.
Ticlopidine hydrochloride is a selective P2Y12 receptor antagonist.
Ticagrelor is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM respectively.
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