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Recent Advances in α1-Adrenoreceptor Antagonists as Pharmacological Tools and Therapeutic Agents

[ Vol. 7 , Issue. 2 ]


Michela Rosini, Maria L. Bolognesi, Dario Giardina, Anna Minarini, Vincenzo Tumiatti and Carlo Melchiorre   Pages 147 - 162 ( 16 )


Native α1-adrenoreceptors (ARs) appear to exist as three different subtypes encoded by three genes, α1A/1a, α1B/1b, and α1D/1d. Historically, the discovery of agents selective for each of the three α1-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, α1-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.


Alpha-1 adrenoreceptors, alpha-1 adrenergic antagonists, quinazolines, benzodioxanes, arylpiperazines, 1,4- dihydropyridines


Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.

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