Structure-Activity Relationships of Histamine H2 Receptor Ligands+

Stefan      Dove; Sigurd      Elz; Roland      Seifert; Armin      Buschauer

doi:10.2174/1389557043403242

Abstract

Recent research on histamine H2 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 H2 receptor-Gsα 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.

Keywords: h2 receptor agonists, h2 receptor antagonists, impromidine analogues, arpromidine, molecular modelling, structure-activity relationships, qsar, site-directed mutagenesis