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Synthesis and pharmacology of potent 5-HT2A receptor agonists which have a partial N-2-methoxybenzyl

Synthesis and pharmacology of potent 5-HT2A receptor agonists which have a partial N-2-methoxybenzyl

  1. Phenoxide
    Synthesis and pharmacology of potent 5-HT2A receptor agonists which have a partial N-2-methoxybenzyl structure - Development of a new structure-activity concept
    Doctorate thesis submitted by Ralf Heim to the Free University of Berlin in 2003. Discusses several novel classes of 5-HT2A agonist featuring an N-2-methoxybenzyl substitution.

    The documents are in german. Due to file size restrictions the references list is uploaded as a separate document.

    Translated opening passage of 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. This structure-activity approach, whereby an N-2-methoxy-N-2-hydroxybenzyl-function 5-HT2A receptor agonist with a primary amine structure a very high potency gives could convincingly be applied to other classes of substances such as tryptamine and phenylethylamine.