An inhibitor of DBH (IC50 = 9 nM for the purified human enzyme); selective for DBH over a panel of 12 enzymes and 13 neurotransmitter receptors (IC50s or Kis = >10 μM); dose-dependently reduces norepinephrine content and increases dopamine content in the mesenteric artery

Nepicastat (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
170151-24-3
Storage:
-20
UN-No:
Non-Hazardous - /

Nepicastat is an inhibitor of dopamine β-hydroxylase (DBH; IC50 = 9 nM for the purified human enzyme).{45348} 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.{45349} Nepicatstat (50 mg/kg) reduces the progressive ratio response for cocaine, but not food or sucrose pellets, in rats.{45350} It also reduces reinstatement of cocaine-seeking behavior induced by cues, yohimbine (Item No. 19869), or foot-shock in rats.  

 

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Description

An inhibitor of DBH (IC50 = 9 nM for the purified human enzyme); selective for DBH over a panel of 12 enzymes and 13 neurotransmitter receptors (IC50s or Kis = >10 μM); 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; attenuates increases in diastolic blood pressure and heart rate induced by preganglionic sympathetic nerve stimulation in pithed spontaneously hypertensive rats at 10 and 30 mg/kg; reduces the progressive ratio response for cocaine, but not food or sucrose pellets, in rats at 50 mg/kg; reduces reinstatement of cocaine-seeking behavior induced by cues, yohimbine, or foot-shock in rats

Formal name: 5-(aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-2H-imidazole-2-thione, monohydrochloride

Synonyms:  RS 25560-197

Molecular weight: 331.8

CAS: 170151-24-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Cardiovascular System|Kidney & Renal Disease||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research

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