Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
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Nerenberg JB, Erb JM, Thompson WJ, Lee HY, Guare JP, Munson PM, Bergman JM, Huff JR, Broten TP, Chang RS, Chen TB, O'Malley S, Schorn TW, Scott AL
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
Bioorg Med Chem Lett. 1998 Sep 22;8(18):2467-72.
- PubMed ID
- 9873563 [ View in PubMed]
- Abstract
Benign prostatic hyperplasia can be managed pharmacologically with alpha-1 adrenergic receptor antagonists. Agents that demonstrate selectivity for the alpha-1a receptor subtype may offer advantages in clinical applications with respect to hypotensive side effects. The N-alkylated saccharins reported here represent a new class of subtype selective alpha-1a adrenergic receptor antagonists which demonstrate potent effects on prostate function in vivo and are devoid of blood pressure side effects.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Terazosin Alpha-1A adrenergic receptor Ki (nM) 2 N/A N/A Details Terazosin Alpha-1A adrenergic receptor Ki (nM) 4.2 N/A N/A Details Terazosin Alpha-1A adrenergic receptor Ki (nM) 2.4 N/A N/A Details Terazosin Alpha-1A adrenergic receptor Ki (nM) 32 N/A N/A Details Terazosin Alpha-1A adrenergic receptor Ki (nM) 2.9 N/A N/A Details Terazosin Alpha-1B adrenergic receptor Ki (nM) 1.2 N/A N/A Details Terazosin Alpha-1D adrenergic receptor Ki (nM) 2 N/A N/A Details