Selective α1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones

✍ Scribed by Philippe G Nantermet; James C Barrow; Harold G Selnick; Carl F Homnick; Roger M Freidinger; Raymond S.L Chang; Stacey S O'Malley; Duane R Reiss; Theodore P Broten; Richard W Ransom; Douglas J Pettibone; Timothy Olah; Carlos Forray

• Book ID: 104364978
• Publisher: Elsevier Science
• Year: 2000
• Tongue: English
• Weight: 144 KB
• Volume: 10
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/s0960-894x(99)00696-4

✦ Synopsis

AbstractÐA series of a 1a 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 ecacy in a prostate contraction model in rats was observed with a few derivatives.