| Bioactivity | ADRA1D receptor antagonist 1 is a potent, selective and orally active α1D adrenoceptor antagonist, with a Ki of 1.6 nM[1]. |
| Target | Ki: 1.6 nM (α1D adrenoceptor) |
| Invitro | 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]. |
| In Vivo | 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: |
| Name | ADRA1D receptor antagonist 1 |
| CAS | 1191908-14-1 |
| Formula | C15H14Cl2N4O |
| Molar Mass | 337.20 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| Reference | [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 Ethe |