195881-94-8
Chemical Structure
(R)-Nepicastat hydrochloride
Synonym(s): (R)-SYN117 hydrochloride; (R)-RS-25560-197 hydrochloride; RS-25560-198 hydrochloride
- CAS No.: 195881-94-8
- Formula:C14H16ClF2N3S
- Molecular Weight:331.81
IUPAC Name: (R)-5-(aminomethyl)-1-(5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)-1,3-dihydro-2H-imidazole-2-thione hydrochloride
InChIKey: DIPDUAJWNBEVOY-HNCPQSOCSA-N
SMILES: S=C1NC=C(CN)N1[C@H]2CC3=C(C(F)=CC(F)=C3)CC2.Cl
Biological Activity: (R)-Nepicastat hydrochloride is the isomer of Nepicastat (HY-13289). Nepicastat (SYN117) is a selective，potent，and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) can cross the blood-brain barrier (BBB)[1][2][3].
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(R)-Nepicastat hydrochloride | (R)-Nepicastat hydrochloride is the isomer of Nepicastat (HY-13289). Nepicastat (SYN117) is a selective，potent，and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) 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. 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]
- [3]. 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]
