FIDUXOSIN
| 中文名称 | FIDUXOSIN |
|---|---|
| 中文同义词 | 化合物 T11286 |
| 英文名称 | Fiduxosin |
| 英文同义词 | 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]- |
| CAS号 | 208993-54-8 |
| 分子式 | C30H29N5O4S |
| 分子量 | 555.65 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 208993-54-8.mol |
| 结构式 |  |
FIDUXOSIN 性质
| 密度 | 1.339±0.06 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 8.40±0.20(Predicted) |
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)
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.
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.