ChemicalBook--->CAS DataBase List--->677773-32-9

677773-32-9

677773-32-9 Structure

677773-32-9 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[form ]

Solid
[color ]

Light yellow to yellow
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H319
[Precautionary statements ]

P264-P280-P305+P351+P338-P337+P313P
Hazard InformationBack 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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