nepicastat hydrochloride monohydrate

Nepicastat hydrochloride monohydrate is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine.

Nepicastat (SYN117) is a selective, potent, and orally active dopamine-beta-hydroxylase inhibitor capable of crossing the blood-brain barrier (BBB), producing concentration-dependent inhibition of bovine and human dopamine-beta-hydroxylase with IC50s of 8.5 nM and 9 nM [1] [2] [3].

Nepicastat hydrochloride (RS-25560-197 hydrochloride) is an effective and specific inhibitor, which is used for bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, respectively.The affinity of Nepicastat for twelve other enzymes and thirteen neurotransmitter receptors is negligible.

(R)-Nepicastat HCl (RS-25560-198 HCl), the R-enantiomer of Nepicastat HCl, is a potent and selective inhibitor with IC50 of 25.1 nM and 18.3 nM for bovine and human dopamine-β-hydroxylase, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors.