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ChemicalBook--->CAS DataBase List--->760173-05-5

760173-05-5

760173-05-5 Structure

760173-05-5 Structure
IdentificationBack Directory
[Name]

(R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione
[CAS]

760173-05-5
[Synonyms]

BIA 5-453
EtaMicastat
(R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione
[Molecular Formula]

C14H15F2N3OS
[MDL Number]

MFCD16619338
[MOL File]

760173-05-5.mol
[Molecular Weight]

311.35
Chemical PropertiesBack Directory
[Boiling point ]

435.3±55.0 °C(Predicted)
[density ]

1.44
[storage temp. ]

Store at -20°C
[solubility ]

Soluble in DMSO
[form ]

powder
[pka]

11.73±0.70(Predicted)
[color ]

white to beige
Hazard InformationBack Directory
[Uses]

Etamicastat (BIA 5-453) 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].
[Biological Activity]

Orally activepotentreversible and peripherally selective dopamine-β-hydroxylase (DBH) inhibitor.
Etamicast at (BIA 5-453) is an orally activepotentreversible and peripherally selective dopamine-β-hydroxylase (DBH) inhibitor th at reduces both systolic (SBP) and diastolic (DBP) blood pressure.
[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).
[storage]

Store at -20°C
[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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