Discovery and Structure-Activity Relationships of 2,5-Dimethoxyphenylpiperidines as Selective Serotonin 5-HT<sub>2A</sub> Receptor Agonists.
Abstract
Classical psychedelics such as psilocybin, lysergic acid diethylamide (LSD), and <i>N,N</i>-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-HT<sub>2A</sub>R), 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-HT<sub>2A</sub>R agonists and detail the structure-activity investigations leading to the identification of LPH-5 [analogue (<i>S</i>)-<b>11</b>] as a selective 5-HT<sub>2A</sub>R agonist with desirable drug-like properties.
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