Medicinal chemical and pharmacological aspects of imidazole-containing histamine H3 receptor antagonists

被引:61
|
作者
Stark, H
Kathmann, M
Schlicker, E
Schunack, W
Schlegel, B
Sippl, W
机构
[1] Goethe Univ Frankfurt, Inst Pharmaceut Chem, Biozentrum, D-60439 Frankfurt, Germany
[2] Univ Bonn, Inst Pharmakol & Toxikol, D-53113 Bonn, Germany
[3] Free Univ Berlin, Inst Pharm, D-14195 Berlin, Germany
[4] Univ Dusseldorf, Inst Pharmazeut Chem, D-40225 Dusseldorf, Germany
[5] Univ Halle Wittenberg, Inst Pharmaceut Chem, D-06120 Halle An Der Saale, Germany
关键词
cipralisant; ciproxifan; clobenpropit; H-3; receptor; imidazole; SCH; 79687; radioligand; thioperamide;
D O I
10.2174/1389557043403107
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The first antagonists known for the histamine H-3 receptor were mono-substituted imidazole-containing compounds like thioperamide. Meanwhile numerous novel leads have been developed possessing improved affinities, selectivities, specificities, and pharmacokinetic properties. Scope and limitations of this promising class are discussed concerning their structure-activity relationships as well as pharmacological and potential therapeutic aspects.
引用
收藏
页码:965 / 977
页数:13
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