| Identification | Back Directory | [Name]
Nepicastat | [CAS]
173997-05-2 | [Synonyms]
SYN117
CS-853
Nepitat
Nepicastat
RS-25560-197
Nepicastat HCl
Nepicastat [inn]
Nepicastat (SYN 117)
Nepicastat (free base) (SYN-117)
SYN117;RS-25560-197;SYN-117;SYN 117
5-(AMinoMethyl)-1-((S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthyl)-4-iMidazoline-2-thione
(S)-5-(Aminomethyl)-1-(5,7-difluoro-1,2,3,4-tetrahydro-naphthalen-2-yl)-1H-imidazole-2(3H)-thi
(S)-5-(Aminomethyl)-1-(5,7-difluoro-1,2,3,4-tetrahydro-naphthalen-2-yl)-1H-imidazole-2(3H)-thione
5-(Aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-2H-imidazole-2-thione
2H-Imidazole-2-thione, 5-(aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-
(S)-5-Aminomethyl-1-(5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)-2,3-dihydro-2-thioxo-1H-imidazole Hydrochloride | [Molecular Formula]
C14H15F2N3S | [MDL Number]
MFCD09837766 | [MOL File]
173997-05-2.mol | [Molecular Weight]
295.35 |
| Chemical Properties | Back Directory | [Boiling point ]
401.8±55.0 °C(Predicted) | [density ]
1.40 | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: ≥ 48 mg/mL (162.52 mM) | [form ]
Powder | [pka]
11.69±0.70(Predicted) |
| Hazard Information | Back Directory | [Uses]
Treatment of congestive heart failure (dopamine β-hydroxylase inhibitor). | [Definition]
ChEBI: Nepicastat is a member of the class of 1,3-dihydroimidazole-2-thiones that is 1,3-dihydro-2H-imidazole-2-thione in which one of the nitrogens is substituted by a 5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl group while the carbon adjacent to it is substituted by an aminomethyl group (the S enantiomer). It is a potent and selective inhibitor of both bovine and human dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine. It has a role as an EC 1.14.17.1 (dopamine beta-monooxygenase) inhibitor. It is a member of tetralins, an organofluorine compound, a primary amino compound and a member of 1,3-dihydroimidazole-2-thiones. | [in vivo]
Nepicastat (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: | Oral administration; three consecutive times, 12 hours apart | | Administration: | 3, 10, 30, 100 mg/kg | | 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. |
| [target]
DBH | [storage]
Store at -20°C |
|
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