Potent and selective dopamine β
-hydroxylase (DBH) inhibitor (IC50
= 9 nM). Selective for DBH over 12 other enzymes. Decreases noradrenaline and increases dopamine levels in tissues and plasma in hypertensive rats. Prevents progressive left ventricular dysfunction in an in vivo
heart failure model. Also potentiates the stimulus effects of cocaine without producing cocaine-like effects in rats. Orally bioavailable.
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Effects of dopamine β-hydroxylase inhibition with nepicastat on the progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure.
Sabbah et al.
Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase.
Stanley et al.
Dopamine β-hydroxylase inhibitors enhance the discriminative stimulus effects of cocaine in rats.
Manvich et al.