Clozapine derived 2,3-dihydro-1H-1,4-and 1,5-benzodiazepines with D4 receptor selectivity:: synthesis and biological testing

被引：36
|
作者：
Hussenether, T [1 ]
Hübner, H [1 ]
Gmeiner, P [1 ]
Troschütz, R [1 ]
机构：
[1] Univ Erlangen Nurnberg, Emil Fischer Ctr, Dept Med Chem, D-91052 Erlangen, Germany
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2004年 / 12卷 / 10期
关键词：
D O I：
10.1016/j.bmc.2004.03.023
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Novel 4-arylpiperazin-l-yl-substituted 2,3-dihydro-1H-1,4- and 1H-1,5-benzodiazepines and their aza-analogues were synthesized as debenzoclozapine derivatives for evaluation as potential D4-ligands. While K-i values of some of the title compounds came within the range of clozapine, they showed an impressively greater selectivity over other dopamine receptor subtypes, especially D2. For the most promising compounds, intrinsic activity and binding properties to serotonin 5-HT1(A) and 5-HT2 were also determined. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2625 / 2637
页数：13
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