| Bioactivity | ADRA1D receptor antagonist 1 (free base) (compound (R)-9s) is an orally active, potent and selective human α1D-adrenoceptor (α1D-AR) antagonist (Ki=1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence. |
| In Vivo | ADRA1D receptor antagonist 1 (free base) (10 µg/kg; p.o.; single) inhibits cyclophosphamide-induced urinary frequency in rats[1].ADRA1D receptor antagonist 1 (free base) (4.4 µg/kg; i.v.; single) inhibits bladder contraction with an IC 30 value of 15 nM in rats[1]. Animal Model: |
| Name | ADRA1D receptor antagonist 1 free base |
| CAS | 1191908-24-3 |
| Formula | C15H13ClN4O |
| Molar Mass | 300.74 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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 Ether-a-go-go-Related Gene (hERG) Liabilities. J Med Chem. 2016 Apr 14;59(7):2989-3002. |