Identification | Back Directory | [Name]
Etamicastat HCl salt | [CAS]
677773-32-9 | [Synonyms]
Etamicastat HCl salt BIA 5-453 hydrochloride Etamicastat hydrochloride | [Molecular Formula]
C14H16ClF2N3OS | [MDL Number]
MFCD32173149 | [MOL File]
677773-32-9.mol | [Molecular Weight]
347.81 |
Hazard Information | Back Directory | [Description]
Etamicastat, also known as BIA 5-453, is a potent, reversible, peripherally selective dopamine β-hydroxylase inhibitor (DBH inhibitor). Chronic dopamine ?-hydroxylase inhibition with etamicastat effectively decreases blood pressure, although does not prevent the development of hypertension in the spontaneously hypertensive rat. | [Uses]
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]. | [in vivo]
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] | Dosage: | 100 mg/kg | Administration: | Administered intraperitoneally | Result: | Led to a significant reduction of noradrenaline levels (36% control) in heart with concomitant increasing in dopamine levels (850% of control). |
Animal Model: | Male Wistar rats[1] | Dosage: | 50 mg/kg (Pharmacokinetic Analysis) | Administration: | Orally administered with at a dose volume of 10 mL/kg | Result: | Oral bioavailability (64%), Cmax (4.9 nM), and (T1/2=3.7 h). |
| [References]
[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. DOI:10.1016/j.ejphar.2014.07.027 [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 Ju |
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