Obiekt

Tytuł: Utilization of cellular models in search for potent metabotropic receptor ligands, basing on the example of adenosine, histamine and cannabinoid receptors

Abstrakt:

Presented thesis describes the development of cell lines, overexpressing adenosine A2A, cannabinoid CB1 and CB2 and histamine H4 receptors. Derived cellular models supplemented available tools to investigate the molecular pharmacology of seven-transmembrane receptors.Within the study, an influence of transfection/transduction method and labeling of receptor with fluorescent protein, on ligand binding parameters was evaluated for adenosine A2A and histamine H4 receptors.Cell lines obtained in current work were additionally used to test 61 derivatives of dialkyl-pyrimidopurinediones for their activity towards the family of adenosine receptors. In the considered group of structures, active compounds were identified (with Ki values in nanomolar and submicromolar concentration range), representing various selectivity to particular receptor subtypes. The obtained results enabled the identification of crucial structural elements of tested compounds, necessary for achievement of high affinity to adenosine receptors.Experiments carried out within the study allowed for confirmation of agonistic activity of Δ9-THC at GPR18 orphan receptor. Moreover, β-arrestin recruitment assay at GPR18 receptor, in connection with CB1R and CB2R radioligand binding assays, developed within the presented thesis, were used for the characterization of 41 derivatives of imidazothiazolone, imidazothiazinone an ; d imidazo-thiazepinone as a potential ligands of cannabinoid receptors subtypes and GPR18 orphan receptor.

Miejsce wydania:

Kraków

Stopień studiów:

2 - studia doktoranckie

Instytucja nadająca tytuł:

Wydział Farmaceutyczny

Promotor:

Kieć-Kononowicz, Katarzyna

Data wydania:

2014

Identyfikator:

oai:dl.cm-uj.krakow.pl:3998

Sygnatura:

ZB-122906

Język:

pol

Prawa dostępu:

nieograniczony

Kolekcje, do których przypisany jest obiekt:

Data ostatniej modyfikacji:

26 cze 2023

Data dodania obiektu:

18 cze 2015

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1 575

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98

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http://dl.cm-uj.krakow.pl:8080/publication/3998

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Nazwa wydania Data
ZB-122906 26 cze 2023
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