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.
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Animal models | spontaneously hypertensive rats (SHRs) |
Formulation | water |
Dosages | 3, 10, 30 or 100 mg/kg |
Administration | p.o. |
Molecular Weight | 331.81 |
Formula | C14H15F2N3S.HCl |
CAS Number | 170151-24-3 |
Solubility (25°C) | DMSO 56 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
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.
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