Nepicastat hydrochloride
Chemical Name: 5-(Aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-2H-imidazole-2-thione hydrochloride
Purity: ≥98%
Biological Activity
Nepicastat hydrochloride is a 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of DA-beta-hydroxylase.
Stanley et al.
Br.J.Pharmacol., 1997;121:1803 -
DA β-hydroxylase inhibitors enhance the discriminative stimulus effects of cocaine in rats.
Manvich et al.
J.Pharmacol.Exp.Ther., 2013;347:564 -
Effects of DA β-hydroxylase inhibition with nepicastat on the progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure.
Sabbah et al.
Circulation, 2000;102:1990
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Citation for Nepicastat hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for Nepicastat hydrochloride include:
1 Citation: Showing 1 - 1
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Synergistic Growth Inhibition of HT-29 Colon and MCF-7 Breast Cancer Cells with Simultaneous and Sequential Combinations of Antineoplastics and CNS Drugs.
Authors: Armando Et al.
Int J Mol Sci 2021;22
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