| 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 ED50 values of fiduxosin is 0.24 mg/kg. |