170151-24-3
Chemical Structure
Nepicastat hydrochloride
Synonym(s): SYN-117 hydrochloride; RS-25560-197 hydrochloride
- CAS No.: 170151-24-3
- Formula:C14H16ClF2N3S
- Molecular Weight:331.81
IUPAC Name: (S)-5-(aminomethyl)-1-(5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)-1,3-dihydro-2H-imidazole-2-thione hydrochloride
InChIKey: DIPDUAJWNBEVOY-PPHPATTJSA-N
SMILES: FC1=CC(F)=C2CC[C@@H](CC2=C1)N3C(CN)=CNC3=S.Cl
Biological Activity: Nepicastat hydrochloride (SYN-117 hydrochloride) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat hydrochloride produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat hydrochloride can cross the blood-brain barrier (BBB)[1][2][3].
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Nepicastat hydrochloride | 99.40% | Nepicastat hydrochloride (SYN-117 hydrochloride) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat hydrochloride produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat hydrochloride can cross the blood-brain barrier (BBB). | ||||||||||||||||||||
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References
- [1]. Beliaev A, et al. Synthesis and biological evaluation of novel, peripherally selective chromanyl imidazolethione-based inhibitors of dopamine beta-hydroxylase.J Med Chem. 2006 Feb 9;49(3):1191-7. [Content Brief]
- [2]. Stanley WC, et al. Cardiovascular effects of nepicastat (RS-25560-197), a novel dopamine beta-hydroxylase inhibitor. J Cardiovasc Pharmacol. 1998 Jun;31(6):963-70. [Content Brief]
- [3]. Stanley WC, et al. Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase. Br J Pharmacol. 1997 Aug;121(8):1803-9. [Content Brief]
