GW 791343 hydrochloride is a P2X7 allosteric modulator (pIC50 = 6.9 - 7.2). 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. GW 791343 hydrochloride exhibits negative allosteric effects at the human P2X(7) receptor but is a positive allosteric modulator of rat P2X(7). GW791343 can significantly affect agonist potency at the P2X(7) receptor by its predominant effect. Further studies, in which single amino acids were exchanged, identified amino acid 95 as being primarily responsible for the differential allosteric effects of GW791343.
|Source||Front Pharmacol (2018). Figure 3.GW 791343|
|Cell Lines||SCN cells|
|Incubation Time||24–48 h|
|Results||In contrast GW791343 (100 nM), a positive allosteric modulator of rat P2X7R, enhanced the amplitude of ATP release rhythm and extracellular ATP accumulation to 144 ± 6% of control levels|
|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.
Identification of regions of the P2X(7) receptor that contribute to human and rat species differences in antagonist effects.
Michel AD, et al. Br J Pharmacol. 2008 Nov;155(5):738-51. PMID: 18660826.
Negative and positive allosteric modulators of the P2X(7) receptor.
Michel AD, et al. Br J Pharmacol. 2008 Feb;153(4):737-50. PMID: 18071294.
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|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.
GW791343 hydrochloride is ahydrochloride salt form of GW791343, which is a non-competitive allosteric modulator of human P2X7 receptor inhibitor with pIC50 of 7.
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