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 via PubMed Central
Summary
AI-generated from the abstractSubstituted tryptamines show varying potency and selectivity at serotonin receptors and the serotonin transporter. Several compounds, including 5-MeO-DMT and 5-MeO-tryptamine, are potent 5-HT2AR agonists, while others like 5-MeO-NMT and bufotenine have lower activity. At 5-HT2CR, 5-MeO-DMT and 5-MeO-tryptamine are also potent, but bufotenine is inactive. Most tryptamines have weak or no activity at 5-HT1AR and the serotonin transporter. The findings indicate that the 5-methoxy substitution enhances 5-HT2AR and 5-HT2CR potency, while the N,N-dimethyl group is important for high efficacy.
Study at a glance
| Characteristics | In vitro assay Peer reviewed |
|---|---|
| Intervention | substituted tryptamines |
| Keywords | Drug design Medicinal chemistry Therapeutics Neuropharmacology: psychopharmacology Cns research |
| Citations | 40 |
| Key finding | 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.