2417288-67-4
2417288-67-4 結(jié)構(gòu)式
基本信息
物理化學(xué)性質(zhì)
常見問題列表
IC50: 25?nM (Human P2X3 receptor), 92?nM (Rat P2X3 receptor)and 126?nM (Guinea pig P2X3 receptor), 1820 nM (Rat P2X2/3 heterotrimeric receptor) and 3450 nM (Guinea pig P2X2/3 heterotrimeric receptor)
P2X3 antagonist 34 (BLU-5937; 500?nM) is able to block αβ-meATP-induced sensitization and firing activity of isolated primary nociceptors in rat dorsal root ganglions (DRGs), through P2X3 homotrimeric receptor antagonism. The sensitizing effect of αβ-meATP and the inhibition of P2X3 antagonist 34 are reversible after washout.
P2X3 antagonist 34 (BLU-5937; 0.3-0?mg/kg, oral administration; male Dunkin Hartley guinea pigs) treatment significantly reduces the histamine-induced enhancement in the number of citric acid-induced coughs in a dose-dependent fashion in a guinea pig cough model.
P2X3 antagonist 34 (BLU-5937; 3 and 30?mg/kg, oral) is also shown to reduce significantly and dose-dependently the ATP-induced enhancement of citric acid-induced coughs in the guinea pig.
| Animal Model: | Male Dunkin Hartley guinea pigs |
| Dosage: | 0.3 mg/kg, 3 mg/kg, 30?mg/kg |
| Administration: | Oral administration |
| Result: | Significantly reduced the histamine-induced enhancement in the number of citric acid-induced coughs in a dose-dependent fashion. |