New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: High affinity ligands for the α₁-adrenoceptor subtypes

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• 作者：Giuseppe Romeo ; Luisa Materia ; Gabriella Marucci ; Maria Modica ; Valeria Pittal&#xe0 ; Loredana Salerno ; Maria Angela Siracusa ; Michela Buccioni ; Piero Angeli ; Kenneth P. Minneman
• 关键词：α ; ₁-Adrenoceptor ; Ligand ; Antagonist ; Synthesis ; α ; _1D-Adrenoceptor subtype
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 December 2006
• 卷：16
• 期：24
• 页码：6200-6203
• 文件大小：167 K

摘要

A number of new pyrimido[5,4-b]indole and [1]benzothieno[3,2-d]pyrimidine derivatives were synthesized and evaluated for their binding and functional properties at α₁-adrenergic receptor (α₁-AR) subtypes. They behaved as potent α₁-AR antagonists. In binding experiments, some of them (RC24 and RC23) showed very high affinity for the α_1D-AR subtype.