ArticlePsychopharmacology2014
Behavioral and neurochemical pharmacology of six psychoactive substituted phenethylamines: mouse locomotion, rat drug discrimination and in vitro receptor and transporter binding and function.
Article in Psychopharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers, 1 of them a synthesis that pooled it.
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Who cites it
38 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Synergistic, multi-level understanding of psychedelics: three systematic reviews and meta-analyses of their pharmacology, neuroimaging and phenomenology.Translational psychiatry · 2024Pooled it
- History, pharmacology and therapeutic mechanisms of 3,4-methylenedioxymethamphetamine (MDMA).British journal of pharmacology · 2026Review
- Short- and Long-Acting Psychedelics: Structure-Activity Relationships, Pharmacology, and Implications for Neuropsychiatric Therapeutics.ACS chemical neuroscience · 2026Review
- The 4-alkyl chain length of 2,5-dimethoxyamphetamines differentially affects in vitro serotonin receptor actions versus in vivo psychedelic-like effects.Molecular psychiatry · 2026Article
- Mind the gap! Addressing unresolved aspects of abuse potential evaluation and scheduling of classic and novel psychedelic drugs.Journal of psychopharmacology (Oxford, England) · 2026Review
- The evolution of N, N-Dimethyltryptamine: from metabolic pathways to brain connectivity.Psychopharmacology · 2025Review
- Toxicodynamic insights of 2C and NBOMe drugs - Is there abuse potential?Toxicology reports · 2025Review
- Locomotor and discriminative stimulus effects of NBOH hallucinogens in rodents.Behavioural pharmacology · 2025Article
- Acute Effects of the Psychedelic Phenethylamine 25I-NBOMe in C57BL/6J Male Mice.International journal of molecular sciences · 2025Article
- 5-hydroxytryptamine 2C/1A receptors modulate the biphasic dose response of the head twitch response and locomotor activity induced by DOM in mice.Psychopharmacology · 2024Article
- Discovery andACS medicinal chemistry letters · 2023Article
- Off-target activity of NBOMes and NBOMe analogs at the µ opioid receptor.Archives of toxicology · 2023Article
- Pharmacologic Activity of Substituted Tryptamines at 5-Hydroxytryptamine (5-HT)The Journal of pharmacology and experimental therapeutics · 2023Article
- Use of the head-twitch response to investigate the structure-activity relationships of 4-thio-substituted 2,5-dimethoxyphenylalkylamines.Psychopharmacology · 2023Article
- Population pharmacokinetic/pharmacodynamic modeling of the psychedelic experience induced by N,N-dimethyltryptamine - Implications for dose considerations.Clinical and translational science · 2022Article
- Molecular Pathways of the Therapeutic Effects of Ayahuasca, a Botanical Psychedelic and Potential Rapid-Acting Antidepressant.Biomolecules · 2022Review
- Effect ofFrontiers in psychiatry · 2022Article
- Discriminative Stimulus Effects of Substituted Tryptamines in Rats.ACS pharmacology & translational science · 2021Article
- New designer phenethylamines 2C-C and 2C-P have abuse potential and induce neurotoxicity in rodents.Archives of toxicology · 2021Article
- Neuronal and peripheral damages induced by synthetic psychoactive substances: an update of recent findings from human and animal studies.Neural regeneration research · 2020Review
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
rationalePsychoactive-substituted phenethylamines 2,5-dimethoxy-4-chlorophenethylamine (2C-C); 2,5-dimethoxy-4-methylphenethylamine (2C-D); 2,5-dimethoxy-4-ethylphenethylamine (2C-E); 2,5-dimethoxy-4-iodophenethylamine (2C-I); 2,5-dimethoxy-4-ethylthiophenethylamine (2C-T-2); and 2,5-dimethoxy-4-chloroamphetamine (DOC) are used recreationally and may have deleterious side effects.
objectivesThis study compares the behavioral effects and the mechanisms of action of these substituted phenethylamines with those of hallucinogens and a stimulant.
methodsThe effects of these compounds on mouse locomotor activity and in rats trained to discriminate dimethyltryptamine, (-)-DOM, (+)-LSD, (±)-MDMA, and S(+)-methamphetamine were assessed. Binding and functional activity of the phenethylamines at 5-HT1A, 5-HT2A, 5-HT2C receptors and monoamine transporters were assessed using cells heterologously expressing these proteins.
resultsThe phenethylamines depressed mouse locomotor activity, although 2C-D and 2C-E stimulated activity at low doses. The phenethylamines except 2C-T-2 fully substituted for at least one hallucinogenic training compound, but none fully substituted for (+)-methamphetamine. At 5-HT1A receptors, only 2C-T-2 and 2C-I were partial-to-full very low potency agonists. In 5-HT2A arachidonic acid release assays, the phenethylamines were partial to full agonists except 2C-I which was an antagonist. All compounds were full agonists at 5-HT2A and 5-HT2C receptor inositol phosphate assays. Only 2C-I had moderate affinity for, and very low potency at, the serotonin transporter.
conclusionsThe discriminative stimulus effects of 2C-C, 2C-D, 2C-E, 2C-I, and DOC were similar to those of several hallucinogens, but not methamphetamine. Additionally, the substituted phenethylamines were full agonists at 5-HT2A and 5-HT2C receptors, but for 2C-T-2, this was not sufficient to produce hallucinogen-like discriminative stimulus effects. Additionally, the 5-HT2A inositol phosphate pathway may be important in 2C-I's psychoactive properties.
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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.