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Updated: Aug 20, 2026

Modeling Ligands into Maps Derived from Electron Cryomicroscopy
Published on: July 19, 2024
Structure-activity relationships of histamine H2 receptor ligands
Stefan Dove1, Sigurd Elz, Roland Seifert
1Institute of Pharmacy, University of Regensburg, D--93040 Regensburg, Germany.
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-Gsalpha 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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