Description: Nepicastat (SYN-117 and RS-25560-197) 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. Dopamine beta-hydroxylase is an enzyme that catalyzes the conversion of dopamine to norepinephrine.Nepicastat has been studied as a possible treatment for congestive heart failure, and appears to be well tolerated.
References: Br J Pharmacol. 1997 Aug;121(8):1803-9; J Cardiovasc Pharmacol. 1998 Jun;31(6):963-70.Related CAS #: 170151-24-3 (HCl); 173997-05-2 (free base); 195881-94-8 (HCl R isomer)