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Species-selective interactions of histamine H2 receptors with guanidine-type agonists: molecular modelling, site-directed mutagenesis and pharmacological analysis

URN to cite this document:
urn:nbn:de:bvb:355-opus-8438
Preuß, Hendrik
Date of publication of this fulltext: 31 Aug 2007 12:01


Abstract (English)

The histamine H2 receptor (H2R) is a biogenic amine receptor that belongs to the class 1 of G protein coupled receptors (GPCR). N-[3-(1H-imidazol-4-yl)propyl]guanidines such as arpromidine are the most potent H2R agonists known so far. Such compounds might be useful as positive inotropic drugs. Recently, less basic N-acylated derivatives with improved pharmacokinetic properties, i.e. oral ...

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Translation of the abstract (German)

Der Histamin-H2-Rezeptor (H2R) gehört zur Klasse 1 G-Protein-gekoppelter Rezeptoren. Arpromidin und strukturverwandte N-[3-(1H-imidazol-4-yl)propyl]guanidine sind die potentesten beschriebenen H2R-Agonisten. Solche Substanzen könnten als positiv inotrope Arzneistoffe therapeutischen Einsatz finden. Die vom Arpromidin abgeleiteten N-Acylguanidine weisen eine deutlich herabgesetzte Basizität auf ...

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