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

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.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2000-08, Vol.10 (15), p.1625-1628
Main Authors: Nantermet, P G, Barrow, J C, Selnick, H G, Homnick, C F, Freidinger, R M, Chang, R S, O'Malley, S S, Reiss, D R, Broten, T P, Ransom, R W, Pettibone, D J, Olah, T, Forray, C
Format: Article
Language:English
Subjects:
Adrenergic alpha-1 Receptor Antagonists
Adrenergic alpha-Antagonists - chemistry
Adrenergic alpha-Antagonists - pharmacology
Animals
Dihydropyridines - chemistry
Dihydropyridines - pharmacology
Rats
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Summary: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.
ISSN:0960-894X