760173-05-5

760173-05-5 structure

Name: Etamicastat
Chemical Name: 4-(2-aminoethyl)-3-[(3R)-6,8-difluoro-3,4-dihydro-2H-chromen-3-yl]-1H-imidazole-2-thione
CAS Number: 760173-05-5
Molecular Formula: C₁₄H₁₅F₂N₃OS
Molecular Weight: 311.35
Catalog: Research Areas Cardiovascular Disease
Create Date: 2018-08-01 17:27:55
Modify Date: 2024-01-14 12:31:17
Etamicastat (BIA 5-453) is a potent and reversible peripheral dopamine-β-hydroxylase (DβH) inhibitor[1].

Name	4-(2-aminoethyl)-3-[(3R)-6,8-difluoro-3,4-dihydro-2H-chromen-3-yl]-1H-imidazole-2-thione
Synonyms	UNII-9X96V6DBU4 Etamitat

Description	Etamicastat (BIA 5-453) is a potent and reversible peripheral dopamine-β-hydroxylase (DβH) inhibitor[1].
Related Catalog	Research Areas >> Cardiovascular Disease
Target	Dopamine-β-hydroxylase (DβH)[1]
In Vivo	Upon intraperitoneal administration to NMRi mice, Etamicastat (100 mg/ kg) leads to a significant reduction of noradrenaline levels (36% control) in heart with concomitant increasing in dopamine levels (850% of control)[2]. Etamicastat (50 mg/kg) is rapidly absorbed into the systemic circulation reaching a maximum concentration at 4 h post-administration, representing 29% of total Etamicastat and quantified metabolites, using AUC0-t as a measure of systemic exposure[2].
References	[1]. Vaz-da-Silva M, et al. Effect of food on the pharmacokinetic profile of Etamicastat (BIA 5-453). Drugs R D. 2011;11(2):127-36. [2]. Loureiro AI, et al. Etamicastat, a new dopamine-ß-hydroxylase inhibitor, pharmacodynamics and metabolism in rat. Eur J Pharmacol. 2014 Oct 5;740:285-94.