Nepicastat (SYN117) is a selective, potent, and orally active dopamine-beta-hydroxylase inhibitor which can cross the blood-brain barrier (BBB). Nepicastat (SYN117) produces concentration-dependent inhibition of bovine and human dopamine-beta-hydroxylase with IC50s of 8.5 nM and 9 nM [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.