Structure-Activity Relationships of Histamine H2 Receptor Ligands+

Authors: Stefan Dove; Sigurd Elz; Roland Seifert; Armin Buschauer

Source: Mini Reviews in Medicinal Chemistry, Volume 4, Number 9, November 2004 , pp. 941-954(14)

Publisher: Bentham Science Publishers

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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-Gs agr

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

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1389557043403242

Affiliations: 1: Institute of Pharmacy, University of Regensburg, D - 93040 Regensburg, Germany.

Publication date: 2004-11-01

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The scope of Mini-Reviews in Medicinal Chemistry will cover all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies.

Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments.