Etamicastat

Modify Date: 2024-01-14 12:31:17

Etamicastat Structure
Etamicastat structure
Common Name Etamicastat
CAS Number 760173-05-5 Molecular Weight 311.35
Density 1.44 Boiling Point 435.308ºC at 760 mmHg
Molecular Formula C14H15F2N3OS Melting Point N/A
MSDS N/A Flash Point 217.067ºC

 Use of Etamicastat


Etamicastat (BIA 5-453) is a potent and reversible peripheral dopamine-β-hydroxylase (DβH) inhibitor[1].

 Names

Name 4-(2-aminoethyl)-3-[(3R)-6,8-difluoro-3,4-dihydro-2H-chromen-3-yl]-1H-imidazole-2-thione
Synonym More Synonyms

 Etamicastat Biological Activity

Description Etamicastat (BIA 5-453) is a potent and reversible peripheral dopamine-β-hydroxylase (DβH) inhibitor[1].
Related Catalog
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.

 Chemical & Physical Properties

Density 1.44
Boiling Point 435.308ºC at 760 mmHg
Molecular Formula C14H15F2N3OS
Molecular Weight 311.35
Flash Point 217.067ºC
Exact Mass 311.09000
PSA 91.87000
LogP 2.82770

 Synthetic Route

 Synonyms

UNII-9X96V6DBU4
Etamitat
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  • DC Chemicals Limited
  • China
  • Product Name: Etamicastat
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  • Purity: 98.0%
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