ADRA1D receptor antagonist 1 is a potent, selective and orally active α1D adrenoceptor antagonist, with a Ki of 1.6 nM[1].
ADRA1D receptor antagonist 1 shows low hERG inhibition[1].
ADRA1D receptor antagonist 1 exhibits higher selectivity for α1D-AR over α1A- and α1B-ARs [1].
ADRA1D receptor antagonist 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. |
[1]. Sakauchi N, et al. Discovery of 5-Chloro-1-(5-chloro-2-(metlsulfonyl)benzyl)-2-imino-1,2-didropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Active α1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ethe