| Identification | Back Directory | [Name]
Nepicastat hydrochloride | [CAS]
170151-24-3 | [Synonyms]
SYN-117 HCl
SYN-117 hydrochloride
Nepicastat HCl, >=99%
Nepicastat (SYN117)HCI
NEPICASTAT HYDROCHLORIDE
Nepicastat (SYN-117) HCl
Nepicastat HCl (SYN-117)
RS-25560-197 hydrochloride)
Nepicastat (SYN-117) hydrochloride
Nepicastat hydrochloride USP/EP/BP
Nepicastat Hydrochloride (SYN-117 hydrochloride
SYN-117 HYDROCHLORIDE;RS-25560-197 HYDROCHLORIDE
Nepicastat HCl (SYN-117),Nepicastat hydrochloride,
RS 25560-197 Nepicastat hydrochloride
4-(aminomethyl)-3-[(2S)-5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]-1H-imidazole-2-thione
(S)-5-(Aminomethyl)-1-(5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)-1H-imidazole-2(3H)-thio
4-(aminomethyl)-3-[(2S)-5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]-1H-imidazole-2-thione,hydrochloride
(S)-5-(AMinoMethyl)-1-(5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)-1H-iMidazole-2(3H)-thione hydrochloride
5-(Aminomethyl)-1-[5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2(S)-yl]-2,3-dihydro-1H-imidazole-2-thione hydrochloride
5-(Aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-2H-imidazole-2-thione hydrochloride | [Molecular Formula]
C14H16ClF2N3S | [MDL Number]
MFCD00954638 | [MOL File]
170151-24-3.mol | [Molecular Weight]
331.812 |
| Chemical Properties | Back Directory | [storage temp. ]
?20°C | [solubility ]
DMSO: soluble10mg/mL, clear | [form ]
powder | [color ]
white to beige | [InChI]
InChI=1/C14H15F2N3S.ClH/c15-9-3-8-4-10(1-2-12(8)13(16)5-9)19-11(6-17)7-18-14(19)20;/h3,5,7,10H,1-2,4,6,17H2,(H,18,20);1H/t10-;/s3 | [InChIKey]
DIPDUAJWNBEVOY-PPHPATTJSA-N | [SMILES]
C(C1=CNC(=S)N1[C@H]1CCC2=C(C=C(F)C=C2C1)F)N.Cl |&1:7,r| |
| Hazard Information | Back Directory | [Description]
Nepicastat is an inhibitor of dopamine β-hydroxylase (DBH; IC50 = 9 nM for the purified human enzyme).1 It is selective for DBH over a panel of 12 enzymes and 13 neurotransmitter receptors (IC50s or Kis = >10 μM). Nepicastat dose-dependently reduces norepinephrine content and increases dopamine content in the mesenteric artery, left ventricle, and cerebral cortex in spontaneously hypertensive rats, as well as in the renal artery, left ventricle, and cerebral cortex in beagle dogs. It attenuates increases in diastolic blood pressure and heart rate induced by preganglionic sympathetic nerve stimulation in pithed spontaneously hypertensive rats when administered orally at doses of 10 and 30 mg/kg.2 Nepicatstat (50 mg/kg) reduces the progressive ratio response for cocaine, but not food or sucrose pellets, in rats.3 It also reduces reinstatement of cocaine-seeking behavior induced by cues, yohimbine (Item No. 19869), or foot-shock in rats. | [Uses]
Nepicastat Hydrochloride is a potent and selective dopamine β-hydrolase inhibitor. Used in cardiovascular treatment where deficiencies in ventricles results in heart failure. | [in vivo]
Nepicastat hydrochloride (SYN-117 hydrochloride) (3-100 mg/kg; p.o.; three consecutive times, 12 hours apart times) produces dose-dependent decreases in noradrenaline content, increases in dopamine content and increases in dopamine/noradrenaline ratio in the artery (mesenteric or renal), left ventricle[3]. | Animal Model: | 15-16 weeks male spontaneously hypertensive rats (SHRs)[3] | | Dosage: | 3, 10, 30, 100 mg/kg | | Administration: | Oral administration; three consecutive times, 12 hours apart | | Result: | Produced dose-dependent decreases in noradrenaline content, increases in dopamine content and increases in dopamine/noradrenaline ratio in the artery (mesenteric or renal), left ventricle and cerebral cortex. |
| [storage]
Store at -20°C | [References]
[1]. stanley wc, li b, bonhaus dw, et al. catecholamine modulatory effects of nepicastat (rs-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase. br j pharmacol, 1997, 121(8): 1803-1809.
[2]. stanley wc, lee k, johnson lg, et al. cardiovascular effects of nepicastat (rs-25560-197), a novel dopamine beta-hydroxylase inhibitor. j cardiovasc pharmacol, 1998, 31(6): 963-970.
[3]. devoto p, flore g, saba p, et al. the dopamine beta-hydroxylase inhibitor nepicastat increases dopamine release and potentiates psychostimulant-induced dopamine release in the prefrontal cortex. addict biol, 2014, 19(4): 612-622. |
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