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ADRA1D receptor agonist 1

Names

[ CAS No. ]:
1191908-14-1

[ Name ]:
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]:

Research Areas >> Endocrinology
Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

[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

Related Compounds