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Title: Multidirectional activity of new histamine and adenosine receptor ligands

Author:

Olejarz-Maciej, Agnieszka

Date:

2024

Type:

Praca doktorska

Abstract:

The multidirectional activity of ligands creates the possibility of more favourable treatment of diseases with a complicated pathomechanism. The functional selectivity showed by the G protein-coupled receptors ligands allows selective interaction with the desired signal transduction pathway resulting in a more favourable activity and safety profile of ligand. The first part of the work focused on determining the effect of H3 (H3R) and H4 (H4R) histamine receptor ligands on various intracellular signalling pathways. The intrinsic activity of H3R and H4R ligands was determined. Among the H4R ligands with a thiophene moiety, compounds showing functional selectivity were found. The second part of the work focused on the search for multi-target ligands with potential use in the treatment of neurodegenerative diseases. The following multi-target activities were considered: H3R affinity and monoamine oxidase B (MAO-B) inhibition or affinity for A1 and A2A adenosine receptors with MAO-B inhibition. The effect of compounds on MAO-B was examined. Good dual activity of H3R - MAO-B was confirmed. Active MAO-B inhibitors have been found in the group of adenosine receptors’ ligands. The obtained results provided important insight into the structure-activity relationship. They should also contribute to the development of new functionally selective and multi-target ligands.

Place of publishing:

Kraków

Level of degree:

2 - studia doktoranckie

Degree discipline:

farmacja ; neurologia

Degree grantor:

Rada Dyscypliny Nauki farmaceutyczne

Promoter:

Kieć-Kononowicz, Katarzyna ; Karcz, Tadeusz

Date issued:

2023

Identifier:

oai:dl.cm-uj.krakow.pl:5140

Call number:

ZB-139866

Language:

eng; pol

Access rights:

tylko w bibliotece

Subject and keywords:

multidirectional activity functional selectivity histamine receptor’s ligands adenosine receptor’s ligands monoamine oxidase B inhibitors

Object collections:

Last modified:

Dec 6, 2024

In our library since:

Jul 11, 2024

Number of object content hits:

8

Number of object content views in PDF format

0

All available object's versions:

http://dl.cm-uj.krakow.pl:8080/publication/5141

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Edition name Date
ZB-139866 Dec 6, 2024

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