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