Nepicastat hydrochloride (SYN117, RS-25560-197) is an inhibitor of dopamine beta-hydroxylase that catalyzes the conversion of dopamine to norepinephrine. Nepicastat hydrochloride shows the selective and concentration-dependent inhibition effects on bovine and human dopamine-beta-hydroxylase activity in vitro. In vivo, Nepicastat hydrochloride increases dopamine content and dopamine/noradrenaline ratio in a dose-dependent manner. Nepicastat hydrochloride also produces the similar effects on noradrenaline, dopamine and dopamine/noradrenaline ratio in tissues and plasma of beagle dogs. Nepicastat is currently in Phase II clinical trials in patients with Posttraumatic Stress Disorder.
|Animal models||spontaneously hypertensive rats (SHRs)|
|Dosages||3, 10, 30 or 100 mg/kg|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 56 mg/mL|
Disulfiram attenuates drug-primed reinstatement of cocaine seeking via inhibition of dopamine β-hydroxylase.
Schroeder JP, et al. Neuropsychopharmacology. 2010 Nov;35(12):2440-9. PMID: 20736996.
Effects of dopamine beta-hydroxylase inhibition with nepicastat on the progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure.
Sabbah HN, et al. Circulation. 2000 Oct 17;102(16):1990-5. PMID: 11034950.
Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase.
Stanley WC, et al. Br J Pharmacol. 1997 Aug;121(8):1803-9. PMID: 9283721.
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