Discovery and Structure–Activity Relationships of 2,5-Dimethoxyphenylpiperidines as Selective Serotonin 5-HT2A Receptor Agonists
Journal of Medicinal Chemistry 2024
Emil M.Rorsted, Anders A Jensen, Gints Šmits, Karla Frydenvang, Jesper L Kristensen

Classical psychedelics such as psilocybin, lysergic acid diethylamide (LSD), and N,N-dimethyltryptamine (DMT) are showing promising results in clinical trials for a range of psychiatric indications, including depression, anxiety, and substance abuse disorder. These compounds are characterized by broad pharmacological activity profiles, and while the acute mind-altering effects can be ascribed to their shared agonist activity at the serotonin 2A receptor (5-HT2AR), their apparent persistent therapeutic effects are yet to be decidedly linked to activity at this receptor. We report herein the discovery of 2,5-dimethoxyphenylpiperidines as a novel class of selective 5-HT2AR agonists and detail the structure-activity investigations leading to the identification of LPH-5 [analogue (S)-11] as a selective 5-HT2AR agonist with desirable drug-like properties.


Atslēgas vārdi
Agonists, Assays, High-performance liquid chromatography, Mixtures Receptors
DOI
10.1021/acs.jmedchem.4c00082
Hipersaite
https://pubs.acs.org/doi/10.1021/acs.jmedchem.4c00082

M.Rorsted, E., Jensen, A., Šmits, G., Frydenvang, K., Kristensen, J. Discovery and Structure–Activity Relationships of 2,5-Dimethoxyphenylpiperidines as Selective Serotonin 5-HT2A Receptor Agonists. Journal of Medicinal Chemistry, 2024, Vol. 67, No. 9, 7224.-7244.lpp. ISSN 0022-2623. Pieejams: doi:10.1021/acs.jmedchem.4c00082

Publikācijas valoda
English (en)
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