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
Journal of Pharmacology and Experimental Therapeutics 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.
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| 3,4-Methylenedioxymethamphetamine and 3,4-methylenedioxyamphetamine destroy serotonin terminals in rat brain: quantification of neurodegeneration by measurement of [3H]paroxetine-labeled serotonin uptake sites. Rat brain | 1987 | Animal experiment | |
| Comparison of the monoamine transporters from human and mouse in their sensitivities to psychostimulant drugs Human and mouse dopamine, norepinephrine, and serotonin transporters expressed in cells | 2006 | In vitro laboratory study |
Citations in the library
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Cites 30
- Psilocybin produces substantial and sustained decreases in depression and anxiety in patients with life-threatening cancer: A randomized double-blind trial Journal of Psychopharmacology November 30, 2016
- Psilocybin with psychological support for treatment-resistant depression: an open-label feasibility study. The Lancet Psychiatry May 17, 2016
- Trial of Psilocybin versus Escitalopram for Depression New England Journal of Medicine April 14, 2021
- Receptor interaction profiles of novel psychoactive tryptamines compared with classic hallucinogens. European Neuropsychopharmacology May 20, 2016
- Human Psychopharmacology of Hoasca, A Plant Hallucinogen Used in Ritual Context in Brazil The Journal of Nervous and Mental Disease February 1, 1996
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