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

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

Volume: 7 Issue: 2

Author(s): Michela Rosini, Maria L. Bolognesi, Dario Giardina, Anna Minarini, Vincenzo Tumiatti and Carlo Melchiorre

Affiliation:

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

Abstract: 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.

Cite this article as:

Rosini Michela, Bolognesi L. Maria, Giardina Dario, Minarini Anna, Tumiatti Vincenzo and Melchiorre Carlo, Recent Advances in α1-Adrenoreceptor Antagonists as Pharmacological Tools and Therapeutic Agents, Current Topics in Medicinal Chemistry 2007; 7 (2) . https://dx.doi.org/10.2174/156802607779318244