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
Mini-Reviews in Medicinal Chemistry
Title: Structure-Activity Relationships of Histamine H2 Receptor Ligands+
Volume: 4 Issue: 9
Author(s): Stefan Dove, Sigurd Elz, Roland Seifert and Armin Buschauer
Affiliation:
Keywords: h2 receptor agonists, h2 receptor antagonists, impromidine analogues, arpromidine, molecular modelling, structure-activity relationships, qsar, site-directed mutagenesis
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.
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Cite this article as:
Dove Stefan, Elz Sigurd, Seifert Roland and Buschauer Armin, Structure-Activity Relationships of Histamine H2 Receptor Ligands+, Mini-Reviews in Medicinal Chemistry 2004; 4 (9) . https://dx.doi.org/10.2174/1389557043403242
DOI https://dx.doi.org/10.2174/1389557043403242 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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