ADRA1D receptor agonist 1

Modify Date: 2024-01-11 11:28:03

ADRA1D receptor agonist 1 Structure
ADRA1D receptor agonist 1 structure
Common Name ADRA1D receptor agonist 1
CAS Number 1191908-14-1 Molecular Weight 337.20
Density N/A Boiling Point N/A
Molecular Formula C15H14Cl2N4O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of ADRA1D receptor agonist 1


ADRA1D receptor agonist 1 (compound (R)-9S) is a potent, selective and orally active α1D adrenoceptor antagonist, with a Ki of 1.6 nM[1].

 Names

Name ADRA1D receptor agonist 1

 ADRA1D receptor agonist 1 Biological Activity

Description ADRA1D receptor agonist 1 (compound (R)-9S) is a potent, selective and orally active α1D adrenoceptor antagonist, with a Ki of 1.6 nM[1].
Related Catalog
Target

Ki: 1.6 nM (α1D adrenoceptor)[1]

In Vitro ADRA1D receptor agonist 1 shows low hERG inhibition[1]. ADRA1D receptor agonist 1 exhibits higher selectivity for α1D-AR over α1A- and α1B-ARs [1].
In Vivo ADRA1D receptor agonist 1 (4.4 µg/kg; i.v.) dose-dependently decreases the non-voiding bladder contractions during the urinary storage phase in rats with BOO[1]. Animal Model: Rat with bladder outlet obstruction (BOO)[1] Dosage: 4.4 µg/kg Administration: Intravenous injection Result: Dose-dependently decreased the non-voiding bladder contractions during urinary storage phase in rats with BOO.
References

[1]. Sakauchi N, et al. Discovery of 5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Active α1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ether-a-go-go-Related Gene (hERG) Liabilities. J Med Chem. 2016 Apr 14;59(7):2989-3002.

 Chemical & Physical Properties

Molecular Formula C15H14Cl2N4O
Molecular Weight 337.20
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