title: Arylpiperazine substituted heterocycles as selective alpha(1a) adrenergic antagonists.
abstract: Antagonists of the alpha(1)-adrenergic receptors (alpha(1)-ARs) are useful for the treatment of benign prostatic hyperplasia. A series of potent and subtype-selective alpha(1a)-AR antagonists has been synthesized, displaying in vitro binding affinity in the low the nanomolar range.
authors.affiliation: Drug Discovery Research, Johnson & Johnson Pharmaceutical Research and Development LLC, Raritan, NJ 08869, USA.
authors.forename: Haripada
authors.initials: H
authors.lastname: Khatuya
authors.forename: Richard H
authors.initials: RH
authors.lastname: Hutchings
authors.forename: Gee-Hong
authors.initials: GH
authors.lastname: Kuo
authors.forename: Virginia L
authors.initials: VL
authors.lastname: Pulito
authors.forename: Linda K
authors.initials: LK
authors.lastname: Jolliffe
authors.forename: Xiaobing
authors.initials: X
authors.lastname: Li
authors.forename: William V
authors.initials: WV
authors.lastname: Murray
mesh_terms: D018674:Adrenergic Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D058668:Adrenergic alpha-1 Receptor Antagonists; D006576:Heterocyclic Compounds, 4 or More Rings / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D007555:Isoxazoles; D010879:Piperazines / Q000138:chemical synthesis / Q000494:pharmacology; D011485:Protein Binding; D018340:Receptors, Adrenergic, alpha-1; D012680:Sensitivity and Specificity; D013329:Structure-Activity Relationship
chemical_list: C547713:ADRA1A protein, human; D018674:Adrenergic Antagonists; D058668:Adrenergic alpha-1 Receptor Antagonists; D006576:Heterocyclic Compounds, 4 or More Rings; D007555:Isoxazoles; D010879:Piperazines; D018340:Receptors, Adrenergic, alpha-1