A Step Forward to Unravel Open Histamine H2 Receptor Questions: Synthesis and Biological Evaluation of Novel H2R Ligands Including Radio- and Fluorescence-Labeled Pharmacological Tools

URN to cite this document:

urn:nbn:de:bvb:355-epub-460910 Copy

DOI to cite this document:

10.5283/epub.46091 Copy

Tropmann, Katharina

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License: Creative Commons Attribution 4.0 PDF (24MB)

Date of publication of this fulltext: 16 Nov 2023 07:52

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Details

Item type:	Thesis of the University of Regensburg (PhD)
Open Access Type:	Primary Publication
Date:	16 November 2023
Referee:	PD Dr. Andrea Strasser
Date of exam:	31 May 2021
Institutions:	Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Keywords:	Histamine H2 receptor, GPCR, radioligand, orthologs, fluorescent ligands, selectivity, bias, carbamoylguanidines, aminothiazoles, aminothiadiazoles, agonists, docking studies, dopamine D3 receptor, dopamine D2long receptor, central nervous system, flow cytometry, confocal microscopy
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:	46091

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Abstract (English)

In summary, in this work new, labeled (radioactive or fluorescent) molecular tools for the H2R with improved kinetic properties were discovered. In addition, an exchange of thiazole with thiadiazole in ligands of the carbamoylguanidine class was found to lead to high-affinity, subtype-, and D2-like receptor-selective H2R agonists. The results of this work represent a very important step for ...

Abstract (English)

In summary, in this work new, labeled (radioactive or fluorescent) molecular tools for the H2R with improved kinetic properties were discovered. In addition, an exchange of thiazole with thiadiazole in ligands of the carbamoylguanidine class was found to lead to high-affinity, subtype-, and D2-like receptor-selective H2R agonists. The results of this work represent a very important step for future studies of H2R agonists of the carbamoylguanidine type in order to get a better understanding the cellular mechanisms of the H2R in general and specifically its function in the CNS (in vivo).

Translation of the abstract (German)

Zusammenfassend wurden in dieser Arbeit neue, markierte (radioaktiv oder fluoreszierend) molekulare Werkzeuge für den H2R mit verbesserten kinetischen Eigenschaften beschrieben. Außerdem wurde gezeigt, dass der Thiazol/Thiadiazol-Austausch in Liganden der Carbamoyguanidin-Klasse zu hochaffinen, subtyp- und D2-like Rezeptor-selektiven H2R Agonisten führt. Die Ergebnisse dieser Arbeit stellen einen ...

Translation of the abstract (German)

Zusammenfassend wurden in dieser Arbeit neue, markierte (radioaktiv oder fluoreszierend) molekulare Werkzeuge für den H2R mit verbesserten kinetischen Eigenschaften beschrieben. Außerdem wurde gezeigt, dass der Thiazol/Thiadiazol-Austausch in Liganden der Carbamoyguanidin-Klasse zu hochaffinen, subtyp- und D2-like Rezeptor-selektiven H2R Agonisten führt. Die Ergebnisse dieser Arbeit stellen einen sehr wichtigen Schritt für zukünftige Untersuchungen von H2R Agonisten vom Carbamoyguanidin-Typ dar, um die zellulären Mechanismen des H2R im Allgemeinen und spezifisch seine Rolle im ZNS (in-vivo) besser zu verstehen.

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Metadata last modified: 16 Nov 2023 07:52

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