Nepicastat (SYN117) 是一种选择性的，有效的，具有口服活性的多巴胺 β 羟化酶(dopamine-beta-Hydroxylase)抑制剂。Nepicastat (SYN117) 对牛 (IC50=8.5 nM) 和人(IC50=9 nM) 多巴胺 β 羟化酶产生浓度依赖性抑制作用。Nepicastat (SYN117) 可越过血脑屏障。

Nepicastat (SYN117) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine ( IC 50 =8.5 nM) and human ( IC 50 =9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) can cross the blood-brain barrier (BBB) [1] [2] [3].

Nepicastat (3-100 mg/kg; p.o.; three consecutive times, 12 hours apart times) produces dose-dependent decreases in noradrenaline content, increases in dopamine content and increases in dopamine/noradrenaline ratio in the artery (mesenteric or renal), left ventricle [3]. Animal Model: 15-16 weeks male spontaneously hypertensive rats (SHRs) [3] Dosage: Oral administration; three consecutive times, 12 hours apart Administration: 3, 10, 30, 100 mg/kg Result: Produced dose-dependent decreases in noradrenaline content, increases in dopamine content and increases in dopamine/noradrenaline ratio in the artery (mesenteric or renal), left ventricle and cerebral cortex.

173997-05-2

C14H15F2N3S

295.35

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years