ArticlePsychopharmacology2014
Interaction of psychoactive tryptamines with biogenic amine transporters and serotonin receptor subtypes.
Article in Psychopharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 53 papers.
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Who cites it
53 citing papers in PubMed, 96 citations in OpenAlex.
- Investigation of the pharmacological and circuit basis for psychedelic drug effects on interval timing in mice.Psychopharmacology · 2026Article
- The Emergence of Isotryptamine Analogs as Novel Serotonergic Agents with Psychotherapeutic Potential.ACS pharmacology & translational science · 2026Review
- Synthesis and Biological Evaluation of 4‑Bromo-ACS omega · 2026Article
- Short- and Long-Acting Psychedelics: Structure-Activity Relationships, Pharmacology, and Implications for Neuropsychiatric Therapeutics.ACS chemical neuroscience · 2026Review
- Serotonin Transporter Blockade Reduces the Psychedelic-Like Effects of 4-Methoxy-ACS chemical neuroscience · 2026Article
- N,N-Dimethyltryptamine (DMT) Acutely Exposed to Mouse Ventral Tegmental Area IJournal of neurochemistry · 2026Article
- Trip killers: Addressing a critical knowledge gap in psychedelic research.Journal of psychopharmacology (Oxford, England) · 2026Review
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- MUC2 shifts the metabolic profiles of commensal bacteria in defined microbial communities.Microbiome research reports · 2026Article
- The ABCs of psychedelics: a preclinical roadmap for drug discovery.Trends in pharmacological sciences · 2025Review
- The evolution of N, N-Dimethyltryptamine: from metabolic pathways to brain connectivity.Psychopharmacology · 2025Review
- Rapid, Open-Source, and Automated Quantification of the Head Twitch Response in C57BL/6J Mice Using DeepLabCut and Simple Behavioral Analysis.ACS pharmacology & translational science · 2025Article
- Rapid, open-source, and automated quantification of the head twitch response in C57BL/6J mice using DeepLabCut and Simple Behavioral Analysis.bioRxiv : the preprint server for biology · 2025Article
- Structural Pharmacology of Bufotenine Derivatives in Activating the 5-HTResearch (Washington, D.C.) · 2025Article
- Serotonin 1A Receptors Modulate Serotonin 2A Receptor-Mediated Behavioral Effects of 5-Methoxy-ACS chemical neuroscience · 2024Article
- Structure-activity relationships of serotonergic 5-MeO-DMT derivatives: insights into psychoactive and thermoregulatory properties.Molecular psychiatry · 2024Article
- Content analysis of Reddit posts about coadministration of selective serotonin reuptake inhibitors and psilocybin mushrooms.Psychopharmacology · 2024Article
- The Human Microbiome-A Physiologic Perspective.Comprehensive Physiology · 2024Review
- A Plea for Nuance: Should People with a Family History of Bipolar Disorder Be Excluded from Clinical Trials of Psilocybin Therapy?Psychedelic medicine (New Rochelle, N.Y.) · 2024Review
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 1 country.
Funding
Abstract
rationaleSynthetic hallucinogenic tryptamines, especially those originally described by Alexander Shulgin, continue to be abused in the USA. The range of subjective experiences produced by different tryptamines suggests that multiple neurochemical mechanisms are involved in their actions, in addition to the established role of agonist activity at serotonin 2A (5-HT₂A) receptors.
objectivesThis study evaluated the interaction of a series of synthetic tryptamines with biogenic amine neurotransmitter transporters and with serotonin (5-HT) receptor subtypes implicated in psychedelic effects.
methodsNeurotransmitter transporter activity was determined in rat brain synaptosomes. Receptor activity was determined using calcium mobilization and DiscoveRx PathHunter assays in HEK293, Gα16-CHO, and CHOk1 cells transfected with human receptors.
resultsTwenty-one tryptamines were analyzed in transporter uptake and release assays, and 5-HT₂A, serotonin 1A (5-HT₁A), and 5-HT₂A β-arrestin functional assays. Eight of the compounds were found to have 5-HT-releasing activity. Thirteen compounds were found to be 5-HT uptake inhibitors or were inactive. All tryptamines were 5-HT₂A agonists with a range of potencies and efficacies, but only a few compounds were 5-HT1A agonists. Most tryptamines recruited β-arrestin through 5-HT₂A activation.
conclusionsAll psychoactive tryptamines are 5-HT₂A agonists, but 5-HT transporter (SERT) activity may contribute significantly to the pharmacology of certain compounds. The in vitro transporter data confirm structure-activity trends for releasers and uptake inhibitors whereby releasers tend to be structurally smaller compounds. Interestingly, two tertiary amines were found to be selective substrates at SERT, which dispels the notion that 5-HT-releasing activity is limited only to primary or secondary amines.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.