An inhibitor of dopamine β-hydroxylase
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Nepicastat (hydrochloride)

Item No. 22126

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-(aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-2H-imidazole-2-thione, monohydrochloride
CAS Number
170151-24-3
Synonyms
  • RS 25560-197
Molecular Formula
C14H15F2N3S • HCl
Formula Weight
331.8
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 2 mg/ml
λmax
267 nm
SMILES
FC1=CC(F)=C(CC[C@H](N2C(CN)=CNC2=S)C3)C3=C1.Cl
InChi Code
InChI=1S/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-;/m0./s1
InChi Key
DIPDUAJWNBEVOY-PPHPATTJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Stanley, W.C., Li, B., Bonhaus, D.W., et al. Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-β-hydroxylase. Br. J. Pharmacol. 121(8), 1803-1809 (1997).

    2. Stanley, W.C., Lee, K., Johnson, L.G., et al. Cardiovascular effects of nepicastat (RS-25560-197), a novel dopamine β-hydroxylase inhibitor. J. Cardiovasc. Pharmacol. 31(6), 963-970 (1998).

    3. Schroeder, J.P., Epps, S.A., Grice, T.W., et al. The selective dopamine β-hydroxylase inhibitor nepicastat attenuates multiple aspects of cocaine-seeking behavior. Neuropsychopharmacology 38(6), 1032-1038 (2013).