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Dimeric histamine H2 receptor agonists as molecular tools and genetically engineered HEK293T cells as an assay platform to unravel signaling pathways of hH1R and hH2R

Plank, Nicole (2016) Dimeric histamine H2 receptor agonists as molecular tools and genetically engineered HEK293T cells as an assay platform to unravel signaling pathways of hH1R and hH2R. PhD, Universität Regensburg.

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Date of publication of this fulltext: 02 May 2016 12:52

Abstract (English)

Previously, our workgroup applied the bivalent ligand approach for the H2R by linking two acylguanidine moieties. This led to highly potent and selective H2R agonists. However, the acylguandines turned out to decompose upon long-term storage in aqueous solution, in particular under alkaline conditions. Based on this preceding work, the medicinal chemistry part of this thesis deals with the ...

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Translation of the abstract (German)

Kürzlich wurden von unserer Arbeitsgruppe bivalente Histamin-H2-Rezeptor (H2R) Liganden, die zwei N(G) acylierte Heteroarylpropylguanidin-Partialstrukturen enthalten, beschrieben. Diese Verbindungen sind hochpotente und selektive H2R Agonisten. Es stellte sich allerdings heraus, dass diese Acylguanidine bei der Lagerung in Lösung, vor allem unter basischen Bedingungen, zur Hydrolyse neigen. ...

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Item type:Thesis of the University of Regensburg (PhD)
Date:2 May 2016
Referee:Prof. Dr. A. Buschauer
Date of exam:30 April 2015
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Keywords:bivalent ligands, human histamine H1R (hH1R), human histamine H2R (hH2R), signaling pathways, HEK293T CRE Luc
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:31862
Owner only: item control page

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