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ID: ALA1131394

Journal: Bioorg Med Chem Lett

Title: Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.

Authors: 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.

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.

CiteXplore: 9873563

DOI: 10.1016/s0960-894x(98)00446-6