An enlightening trip through psychedelic and purinergic signaling.

Pottie, Eline
Faculteit Farmaceutische Wetenschappen
Vakgroep Bioanalyse
Master in Drug Development, Ghent University (Magna cum laude), 2015-2017 Bachelor in Pharmaceutical Sciences, Ghent University, 2012-2015 Latin-Sciences, Sint-Jozefsinstituut, Ternat, 2006-2012
Academische graad
Doctor in de farmaceutische wetenschappen
Taal proefschrift
Vertaling titel
Een verhelderende trip doorheen psychedelische en purinerge signalisatie.
Prof. dr. Christophe Stove, UGent-Bioanalyse
Prof. dr. Serge Van Calenbergh, UGent-Geneesmiddelenleer - Prof. dr. Koen Raemdonck, UGent-Geneesmiddelenleer - Prof. dr. Mette Rosenkilde, University of Copenhagen - Prof. dr. Alain Labro, UGent-Faculteit Geneeskunde en Gezondheidswetenschappen - Dr. Julien Hanson, Université de Liège - Dr. Dino Lüthi, University of Basel

Korte beschrijving

Recent years have witnessed an increasing need for sensitive in vitro techniques to characterize the interaction of ligands with respective G protein-coupled receptors (GPCRs) to keep up with pharmacological insights. Phenomena of particular interest include the determination of structure-activity relationships (SAR) in diverging signaling pathways, the potentially biased agonism of ligands between these pathways, and the possible occurrence of inverse agonism. Furthermore, in vitro bioassays have been described to be applicable for the activity-based detection of new psychoactive substances (NPS) in biological samples, based on the particular activity of a substance rather than on its specific structure. In this thesis, luminescence-based bioassays have been developed to address questions in two contexts, comprised in part A (psychedelic signaling) and part B (purinergic signaling). Part A of this thesis focuses on the development of in vitro assays for the activity-based detection and functional characterization of (psychedelic) agonists of the serotonin 2A receptor (5-HT2AR). The 5-HT2AR is the main pharmacological target of serotonergic psychedelics, a substance group of which a substantially expanding number of compounds appeared on the drug market as NPS throughout the past few years, but which may also have therapeutic potential. Main issues encountered are the difficult detection and the poor characterization of these substances. Part B describes in vitro assays for the characterization of pharmacological phenomena at certain purinergic receptors, including the assessment of biased and inverse agonism at the A3 adenosine receptor (A3AR), and the assessment of molecular determinants of arrestin recruitment at the P2Y2 receptor (P2Y2R). Overall, the bioassays generated and applied in this thesis resulted in ‘An enlightening trip through psychedelic and purinergic signaling’, and prove(d) to be useful to address a variety of pharmacological questions.


Maandag 30 mei 2022, 18:00
Faculteit Farmaceutische Wetenschappen - Auditorium B - Andreas Vesalius, Ottergemsesteenweg 460, 9000 Gent
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