产品
编 号:F106890
分子式:C31H33NO7
分子量:531.6
产品类型
结构图
CAS No: 127308-98-9
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生物活性:
Zamifenacin fumarate (UK-76654 fumarate) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome.
体内研究:
Zamifenacin exhibits moderate oral bioavailability (mouse 26%, rat 64%, dog 100%) and Cmax (mouse 92, rat 905, dog 416 ng/mL) following oral administration (mouse 13.2, rat 20 and, dog 5 mg/kg). Zamifenacin exhibits terminal elimination half-lives (mouse 2.1, rat 6.0 and, dog 1.1 h) due to high plasma clearance (68, 35, and 39 mL/min/kg respectively combined with large volumes of distribution (12.5, 19.0, and 3.5 L/kg respectively) following intravenous administration (mouse 5.3, rat 5.0 and, dog 1.0 mg/kg).Animal Model:Male CDl mice (mean weight 23 g)
Dosage:5.3 mg/kg for i.v.; 13.2 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous administration and oral administration
Result:Oral bioavailability (26%), Cmax (92 ng/mL), T1/2 (1.1 h).
Animal Model:Male and female CD rats (mean weight 210 g)
Dosage:5.0 mg/kg for i.v.; 20 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous administration and oral administration
Result:Oral bioavailability (64%), Cmax (905 ng/mL), T1/2 (6.0 h).
Animal Model:Male and two female beagle dogs (13-16 kg)
Dosage:1.0 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous administration and oral administration
Result:Oral bioavailability (100%), Cmax (416 ng/mL), T1/2 (1.1 h).