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

页码：941 / 954

页数：14

共 162 条

[41] (IMIDAZOLYLPHENYL)FORMAMIDINES - A STRUCTURALLY NOVEL CLASS OF POTENT HISTAMINE H-2-RECEPTOR ANTAGONISTS [J].