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Pharmacologic Activity of Substituted Tryptamines at 5-Hydroxytryptamine (5-HT)2A Receptor (5-HT2AR), 5-HT2CR, 5-HT1AR, and Serotonin Transporter.

Laura B. Kozell, Amy J. Eshleman, Tracy L. Swanson, Shelley H. Bloom, Katherine M. Wolfrum, Jennifer L. Schmachtenberg, Randall J. Olson, Aaron Janowsky, Atheir I. Abbas

J Pharmacol Exp Ther January 20, 2023 DOI: 10.1124/jpet.122.001454 (opens in new tab)

Study at a glance

AI-extracted from the abstract
Characteristics In vitro assay Peer reviewed
Intervention substituted tryptamines
Topics Serotonin
Keywords Drug design Medicinal chemistry Therapeutics Neuropharmacology: psychopharmacology Cns research Neurobiology Brain chemistry Serotonergic system Receptor binding Tryptamines: indoleamines Serotonin analogs
Citations 40
Key points 5-methoxy-substituted tryptamines, particularly 5-MeO-DMT and 5-MeO-tryptamine, are potent agonists at 5-HT2AR and 5-HT2CR, with weak activity at 5-HT1AR and the serotonin transporter.

Abstract

Pharmacologic Activity of Substituted Tryptamines at 5-Hydroxytryptamine (5-HT)2A Receptor (5-HT2AR), 5-HT2CR, 5-HT1AR, and Serotonin Transporter.