BLU-5937
- CAS号:2417288-67-4
- 英文名:1-Piperidinecarboxylic acid, 3-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (3S)-
- 中文名:BLU-5937
- CBNumber:CB58186525
- 分子式:C24H26F2N4O3
- 分子量:456.48
- MOL File:2417288-67-4.mol
- 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
BLU-5937性质、用途与生产工艺
- 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。
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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)
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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.
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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.
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- 国家：美国
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- 国家：美国
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