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208993-54-8

中文名称 FIDUXOSIN
英文名称 Fiduxosin
CAS 208993-54-8
分子式 C30H29N5O4S
分子量 555.65
MOL 文件 208993-54-8.mol
208993-54-8 结构式 208993-54-8 结构式

基本信息

中文别名
化合物 T11286
英文别名
Fiduxosin
3-[4-[(3aR,9bR)-9-methoxy-3,3a,4,9b-tetrahydro-1H-chromeno[3,4-c]pyrrol-2-yl]butyl]-8-phenyl-1H-pyrazino[1,2]thieno[3,4-b]pyrimidine-2,4-dione
Pyrazino[2',3':4,5]thieno[3,2-d]pyrimidine-2,4(1H,3H)-dione, 8-phenyl-3-[4-[(3aR,9bR)-1,3a,4,9b-tetrahydro-9-methoxy[1]benzopyrano[3,4-c]pyrrol-2(3H)-yl]butyl]-

物理化学性质

密度1.339±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度溶于二甲基亚砜
酸度系数(pKa)8.40±0.20(Predicted)

常见问题列表

生物活性
Fiduxosin 是一种 α1-adrenoceptor 拮抗剂,对 α1a-adrenoceptor,α1b-adrenoceptor 和 α1d-adrenoceptor 的 Ki 值分别为 0.160 nM,24.9 nM 和 0.920 nM。
靶点

Ki: 0.16 nM (α1a-adrenoceptor), 24.9 nM (α1b- adrenoceptor), 0.92 nM (α1d-adrenoceptor), 92 nM (Human α2a-adrenoceptor), 22 nM (Human α2c-adrenoceptor), 21 nM (Rat α2b-adrenoceptor), 29 nM (Rat 5HT1A receptor)

体外研究

Fiduxosin displays low affinity for other adrenoceptors, including cloned human α2a- (92 nM) and α2c-adrenoceptors (22 nM) and rat neonatal lung α2b-adrenoceptors (21 nM), in addition to β-adrenoceptors (2-5 μM). Fiduxosin also has low affinity for 5HT1A receptors in rat cortex (29 nM) compared with its affinity at α1a-adrenoceptors (0.16 nM). Fiduxosin antagonizes competitively PE-induced responses with a pA2 value of 7.58, in the rabbit urethra.

体内研究

Fiduxosin (30, 100, and 300 μg/kg, i.v.) antagonizes IUP responses to i.v. EPI in anesthetized dogs. Fiduxosin (178, 592, and 1780 μg/kg, i.v.) elicits transient effects on blood pressure, with no effect of the lowest dose on MAP in spontaneously hypertensive rats (SHR). Fiduxosin (3 μmol/kg or 1780 μg/kg i.v.) slightly reduces MAP, but head-up tilt causes further diminution of MAP at only the 15-min observation with minimal additional changes in MAP at times ≥30 min postdosing in SHR. Fiduxosin (0.1, 0.3, 1.0, and 3.0 mg/kg p.o.) blocks prostatic intraurethral pressure (IUP) responses to a greater extent than MAP responses. The IUP ED 50 values of fiduxosin is 0.24 mg/kg.

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