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

Preuß, Hendrik (2007) Species-selective interactions of histamine H2 receptors with guanidine-type agonists: molecular modelling, site-directed mutagenesis and pharmacological analysis. PhD, Universität Regensburg.

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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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Item type:Thesis of the University of Regensburg (PhD)
Date:30 August 2007
Referee:Prof. Dr. Armin Buschauer
Date of exam:9 July 2007
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Classification:
NotationType
87.15.ByCCS
87.14.EeCCS
87.15.HeCCS
87.15.AaCCS
Keywords:Histamin , Wirkstoff-Rezeptor-Bindung , Molekulardynamik , Molekulardesign , Punktmutation , Histamin-H2-Rezeptor , Spezies-Selektivität , G-Protein-gekoppelter Rezeptor , Fusionsprotein , Sf9-Insektenzellen , histamine H2 receptor , species-selectivity , G protein coupled receptor , site-directed mutagenesis , molecular dynamics
Dewey Decimal Classification:500 Science > 540 Chemistry & allied sciences
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Item ID:10580
Owner only: item control page

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