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Bioorg Med Chem Lett. 2000 Aug 7;10(15):1625-8.

Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.

Author information

1
Department of Medicinal Chemistry, Merck & Co., West Point, PA 19486, USA. philippe_nantermet@merck.com

Abstract

A series of alpha1a receptor antagonists derived from a 4-aryl-3,4-dihydropyridine-2-one heterocycle is disclosed. Potency in the low nanomolar to picomolar range along with high selectivity was obtained. In vivo efficacy in a prostate contraction model in rats was observed with a few derivatives.

PMID:
10937710
DOI:
10.1016/s0960-894x(99)00696-4
[Indexed for MEDLINE]

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