222318-55-0
中文名稱(chēng)
222318-55-0
英文名稱(chēng)
Pyrrolo[2,3-c]azepine-4,8(1H,5H)-dione, 1-[4-[4-(4-fluorobenzoyl)-1-piperidinyl]butyl]-6,7-dihydro-7-methyl-, 4-oxime, (4E)-
CAS
222318-55-0
分子式
C25H31FN4O3
分子量
454.54
MOL 文件
222318-55-0.mol
222318-55-0 結(jié)構(gòu)式
基本信息
中文別名
化合物 T12596 英文別名
(4E)-SUN9221Pyrrolo[2,3-c]azepine-4,8(1H,5H)-dione, 1-[4-[4-(4-fluorobenzoyl)-1-piperidinyl]butyl]-6,7-dihydro-7-methyl-, 4-oxime, (4E)-
物理化學(xué)性質(zhì)
沸點(diǎn)661.7±55.0 °C(Predicted)
密度1.29±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)11.20±0.20(Predicted)
常見(jiàn)問(wèn)題列表
生物活性
(4E)-SUN9221 是一種有效的 α1-adrenergic receptor 和 5-HT2 receptor 拮抗劑，具有抗高血壓和抗血小板聚集的功效。靶點(diǎn)
|
5-HT 2 Receptor
|
α1
|
體外研究
(4E)-SUN9221 potently inhibits collagen-, ADP- and epinephrine-induced platelet aggregation, with IC 50 s of 10 nM, 35 nM, 14 nM, respectively, in human platelet-rich plasma (PRP). (4E)-SUN9221 displays potent α1-adrenergic antagonist activity (pA2 =8.89±0.21) and 5-HT2 antagonist activity (pA2 =8.74±0.22).
體內(nèi)研究
(4E)-SUN9221 (1, 3, 10 mg/kg, p.o.) reduces the blood pressure in a dose-dependent manner in conscious spontaneously hypertensive rats (SHR). (4E)-SUN9221 (3 mg/kg) exhibits antihypertensive activity in SHR.