Selective α(1a) adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones

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

Research output: Contribution to journalArticlepeer-review


A series of α(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 efficacy in a prostate contraction model in rats was observed with a few derivatives. (C) 2000 Elsevier Science Ltd. All rights reserved.

Original languageEnglish (US)
Pages (from-to)1625-1628
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number15
StatePublished - Aug 7 2000
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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