Structure-activity relationships of histamine H2 receptor ligands

被引:31
|
作者
Dove, S
Elz, S
Seifert, R
Buschauer, A [1 ]
机构
[1] Univ Regensburg, Inst Pharm, D-93040 Regensburg, Germany
[2] Univ Kansas, Dept Pharmacol & Toxicol, Lawrence, KS 66045 USA
关键词
H-2 receptor agonists; H-2 receptor antagonists; impromidine analogues; arpromidine; molecular modelling; structure-activity relationships; QSAR; site-directed mutagenesis;
D O I
10.2174/1389557043403242
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Recent research on histamine H-2 receptor agonists was focused on quantitative structure-activity relationships and receptor models explaining the activity of imidazolylpropylguanidines. Their selectivity for guinea pig vs. human isoforms was investigated using H-2 receptor-G(salpha) fusion proteins and attributed to amino acid differences in transmembrane domains 1 and 7. New antagonists result from approaches to improve pharmacokinetic properties and to design hybrid drugs which additionally have gastroprotective or anti H. pylori activity.
引用
收藏
页码:941 / 954
页数:14
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