2417288-67-4

中文名称 BLU-5937

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)-

CAS 2417288-67-4

分子式 C24H26F2N4O3

分子量 456.48

MOL 文件 2417288-67-4.mol

2417288-67-4 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

化合物 T10560

英文别名

1-Piperidinecarboxylic acid, 3-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (3S)-

物理化学性质

密度1.34±0.1 g/cm3(Predicted)

酸度系数(pKa)13.53±0.46(Predicted)

形态Solid

颜色Off-white to light yellow

常见问题列表

生物活性

P2X3 antagonist 34 是一种有效的，选择性的，口服活性的 P2X3 同型三聚体受体拮抗剂，对人 P2X3，大鼠 P2X3 和豚鼠 P2X3 受体的 IC50 分别为 25 nM，92 nM 和 126 nM。P2X3 antagonist 34 对人，大鼠和豚鼠 P2X2/3 异三聚体受体的活性较低。P2X3 antagonist 34 具有很强的镇咳作用。

靶点

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)

体外研究

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.

体内研究

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.