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
来源：
MINI-REVIEWS IN MEDICINAL CHEMISTRY | 2004年 / 4卷 / 09期
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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