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Abstract
Serotonin 2A (5-HT2A) receptors play a central role in triggering hallucinations and in the development of psychological disorders such as schizophrenia and depression. In addition, the 5-HT2A receptor subtype is believed to be important in influencing perception and emotion. Subtype-selective compounds with (partial) agonistic effects on 5-HT2A receptors are used in basic biomedical research as an important experimental tool for the study and understanding of complex physiological and pathophysiological processes, in which the neurotransmitter serotonin (5-HT) is involved.
Based on an unexpected partial agonistic action of a molecular fragment of the classic 5-HT2A receptor antagonist ketanserin, this dissertation discusses the development of structure-activity relationships of a class of 3-(2-aminoethyl)-2,4(1H, 3H)-quinazolinediones developed as 5-HT2A receptor agonists.
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