Dopamine/serotonin receptor ligands.: Part 17:: A cross-target SAR approach:: Affinities of azecine-styled ligands for 5-HT2A versus D1 and D2 receptors

被引：8
|
作者：
Enzensperger, Christoph [1 ]
Goernemann, Tilo [2 ]
Pertz, Heinz H. [2 ]
Lehmann, Jochen [1 ]
机构：
[1] Univ Jena, Inst Pharm, Lehrstuhl Pharmazeut Med Chem, D-07743 Jena, Germany
[2] Free Univ Berlin, Inst Pharm, D-14195 Berlin, Germany
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 13期
关键词：
dopamine; serotonin; receptor ligand; azecine; cross-target SAR; protein-ligand interaction;
D O I：
10.1016/j.bmcl.2008.04.081
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Dibenzo- and benzindolo-azecines represent a novel class of high-affinity dopamine receptor antagonists. To further characterize these drugs as potential neuroleptics, we selected a set of azecine derivatives and ring expanded homologues and we measured their antagonist activity at the 5-HT(2A) receptor in the porcine coronary artery. SARs found for the 5-HT(2A) receptor resemble those for the D(1) but not the D(2) receptor. The protein-ligand interactions were discussed with respect to the different binding pockets. (c) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3809 / 3813
页数：5
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