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GW 791343 dihydrochloride 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.
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Source | Front Pharmacol (2018). Figure 3.GW 791343 |
| Method | Immunohistochemistry | |
| Cell Lines | SCN cells | |
| Concentrations | 5 μM | |
| 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 |
| Molecular Weight | 447.35 |
| Formula | C20H24F2N4O.2HCl |
| CAS Number | 1019779-04-4 |
| Solubility (25°C) | DMSO 32 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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