Nepicastat (SYN-117) HCl 170151-24-3

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Molecular Weight:

331.81 Nepicastat (SYN-117) HCl is a potent and selective inhibitor of both bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors. Phase 2.






Biological Activity


In vitro, Nepicastat hydrochloride shows the selective and
concentration-dependent inhibition effects on bovine and human
dopamine-beta-hydroxylase activity with IC50 of 8.5 nM and 9.0 nM,
respectively. While Nepicastat hydrochloride has negligible affinity for
twelve Other enzymes and thirteen neurotransmitter receptors.


In the artery, left ventricle and cerebral cortex of spontaneously
hypertensive rats (SHRs), Nepicastat hydrochloride reduces noradrenaline
content, and increases dopamine content and dopamine/noradrenaline
ratio in a dose-dependent manner. In addition, Nepicastat hydrochloride
also produces the similar effects on noradrenaline, dopamine and
dopamine/noradrenaline ratio in tissues and plasma of beagle dogs.


In inactin-anesthetized SHRs, Nepicastat hydrochloride (3 mg/kg, i.v.)
produces the antihypertensive effects and causes a significant decrease
in renal vascular resistance (38%) and an increase in renal blood flow
(22%).

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Product Categories : Metabolism > Hydroxylase Inhibitor