Etamicastat hydrochloride (BIA 5-453 hydrochloride) 是一种有效且可逆的多巴胺 β-羟化酶 (DBH) 抑制剂，IC50 值为 107 nM。可用于心血管疾病的研究。
Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a potent and reversible dopamine-β-hydroxylase (DBH) inhibitor with an IC50 value of 107 nM[1]. Etamicastat can be used in the research of cardiovascular diseases[2].
Etamicastat blocks the hERG current amplitude with an IC50 value of 44 μg/mL (141 μM)[2].
Etamicastat (100 mg/kg; administered intraperitoneally) leads to a significant reduction of noradrenaline levels in heart with concomitant increasing in dopamine levels[1].Etamicastat (50 mg/kg; a single oral administration) exhibits moderate oral bioavailability (64%), Cmax (4.9 nM), and terminal elimination half-lives (T1/2=3.7 h) in male Wistar rats[1]. Animal Model: NMRi mice[1]
[1]. Loureiro AI, et al. Etamicastat, a new dopamine-?-hydroxylase inhibitor, pharmacodynamics and metabolism in rat. Eur J Pharmacol. 2014 Oct 5;740:285-94. [2]. ManuelVaz-da-Silva, et al. Cardiac safety profile of etamicastat, a novel peripheral selective dopamine-β-hydroxylase inhibitor in non-human primates, human young and elderly healthy volunteers and hypertensive patients. IJC Metabolic & Endocrine. 2015 Jun; (7): 10-24
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