BLU-5937
| 中文名称 | BLU-5937 |
|---|---|
| 中文同义词 | 化合物 T10560 |
| 英文名称 | 1-Piperidinecarboxylic acid, 3-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (3S)- |
| 英文同义词 | 1-Piperidinecarboxylic acid, 3-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (3S)- |
| CAS号 | 2417288-67-4 |
| 分子式 | C24H26F2N4O3 |
| 分子量 | 456.48 |
| EINECS号 | |
| 相关类别 | 医药原料 |
| Mol文件 | 2417288-67-4.mol |
| 结构式 |  |
BLU-5937 性质
| 密度 | 1.34±0.1 g/cm3(Predicted) |
|---|---|
| 酸度系数(pKa) | 13.53±0.46(Predicted) |
| 形态 | 固体 |
| 颜色 | 米白色至浅黄色 |
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. |