title: Recent advances in alpha1-adrenoreceptor antagonists as pharmacological tools and therapeutic agents.
abstract: Native alpha(1)-adrenoreceptors (ARs) appear to exist as three different subtypes encoded by three genes, alpha(1A/1a), alpha(1B/1b), and alpha(1D/1d). Historically, the discovery of agents selective for each of the three alpha(1)-AR subtypes has been an active area of medicinal chemistry research because of the wide number of possible therapeutic applications. Initially introduced for the management of hypertension, alpha(1)-AR antagonists have, in fact, become increasingly common in the treatment of benign prostatic hyperplasia (BPH), and are effective therapeutic tools, when characterized by an appropriate uroselective profile. The majority of these derivatives display a competitive mechanism of action and belong to a variety of structural classes, but this review is focused on compounds belonging to the quinazoline, benzodioxane, arylpiperazine, and 1,4-dihydropyridine classes.
authors.affiliation: Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
authors.forename: Michela
authors.initials: M
authors.lastname: Rosini
authors.forename: Maria L
authors.initials: ML
authors.lastname: Bolognesi
authors.forename: Dario
authors.initials: D
authors.lastname: Giardinà
authors.forename: Anna
authors.initials: A
authors.lastname: Minarini
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Tumiatti
authors.forename: Carlo
authors.initials: C
authors.lastname: Melchiorre
mesh_terms: D058668:Adrenergic alpha-1 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D004095:Dihydropyridines / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D004146:Dioxanes / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D010879:Piperazines / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D011799:Quinazolines / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D018340:Receptors, Adrenergic, alpha-1 / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D058668:Adrenergic alpha-1 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists; D004095:Dihydropyridines; D004146:Dioxanes; D010879:Piperazines; D011799:Quinazolines; D018340:Receptors, Adrenergic, alpha-1; C038806:1,4-dihydropyridine