Structure-Activity Relationships of Histamine H2 Receptor Ligands+

Author(s): Stefan Dove, Sigurd Elz, Roland Seifert, Armin Buschauer

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 4 , Issue 9 , 2004

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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

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Article Details

Year: 2004
Page: [941 - 954]
Pages: 14
DOI: 10.2174/1389557043403242
Price: $65

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