Prazosin-related compounds. Effect of transforming the piperazinylquinazoline moiety into an aminomethyltetrahydroacridine system on the affinity for α1- …

…, E Poggesi, A Leonardi, C Melchiorre

Index: Rosini, Michela; Antonello, Alessandra; Cavalli, Andrea; Bolognesi, Maria L.; Minarini, Anna; Marucci, Gabriella; Poggesi, Elena; Leonardi, Amedeo; Melchiorre, Carlo Journal of Medicinal Chemistry, 2003 , vol. 46, # 23 p. 4895 - 4903

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Citation Number: 36

Abstract

In a search for structurally new α1-adrenoreceptor (α1-AR) antagonists, prazosin (1)-related compounds 2-11 were synthesized and their affinity profiles were assessed by functional experiments in isolated rat vas deferens (α1A), spleen (α1B), and aorta (α1D) and by binding assays in CHO cells expressing human cloned α1-AR subtypes. Transformation of the piperazinylquinazoline moiety of 1 into an aminomethyltetrahydroacridine system ...