ArticleJournal of psychopharmacology (Oxford, England)2019
Comparison of the behavioral effects of mescaline analogs using the head twitch response in mice.
Article in Journal of psychopharmacology (Oxford, England), 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 23 citations in OpenAlex.
- 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
- Serotonin 2C receptors are also important in head-twitch responses in male mice.Psychopharmacology · 2025Article
- Chemical Reactivity Parameters to Analyze Psychedelics: How Do We Explain the Potency of the Drugs?ACS omega · 2024Article
- Structure-activity relationships of serotonergic 5-MeO-DMT derivatives: insights into psychoactive and thermoregulatory properties.Molecular psychiatry · 2024Article
- Discovery and Structure-Activity Relationships of 2,5-Dimethoxyphenylpiperidines as Selective Serotonin 5-HTJournal of medicinal chemistry · 2024Article
- The Bright Side of Psychedelics: Latest Advances and Challenges in Neuropharmacology.International journal of molecular sciences · 2023Review
- Use of the head-twitch response to investigate the structure-activity relationships of 4-thio-substituted 2,5-dimethoxyphenylalkylamines.Psychopharmacology · 2023Article
- Automated Detection of Psychedelic-Induced Head-Twitch Response in Mice.Methods in molecular biology (Clifton, N.J.) · 2023Article
- Receptor Interaction Profiles of 4-Alkoxy-3,5-Dimethoxy-Phenethylamines (Mescaline Derivatives) and Related Amphetamines.Frontiers in pharmacology · 2021Article
- Pharmacological and biotransformation studies of 1-acyl-substituted derivatives of d-lysergic acid diethylamide (LSD).Neuropharmacology · 2020Article
- Automated detection of the head-twitch response using wavelet scalograms and a deep convolutional neural network.Scientific reports · 2020Article
- Correlation between the potency of hallucinogens in the mouse head-twitch response assay and their behavioral and subjective effects in other species.Neuropharmacology · 2020Article
- Return of the lysergamides. Part V: Analytical and behavioural characterization of 1-butanoyl-d-lysergic acid diethylamide (1B-LSD).Drug testing and analysis · 2019Article
- Receptor Interaction Profiles of 4-Alkoxy-Substituted 2,5-Dimethoxyphenethylamines and Related Amphetamines.Frontiers in pharmacology · 2019Article
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 3 countries.
Funding
Abstract
backgroundIn recent years, there has been increasing scientific interest in the effects and pharmacology of serotonergic hallucinogens. While a large amount of experimental work has been conducted to characterize the behavioral response to hallucinogens in rodents, there has been little systematic investigation of mescaline and its analogs. The hallucinogenic potency of mescaline is increased by α-methylation and by homologation of the 4-methoxy group but it not clear whether these structural modifications have similar effects on the activity of mescaline in rodent models.
methodsIn the present study, the head twitch response (HTR), a 5-HT
resultsTMA induced the HTR and was twice as potent as mescaline. For both mescaline and TMA, replacing the 4-methoxy substituent with an ethoxy or propoxy group increased potency in the HTR assay. By contrast, although TMA-2 also induced the HTR with twice the potency of mescaline, potency was not altered by homologation of the 4-alkoxy group in TMA-2.
conclusionsThe potency relationships for these compounds in mice closely parallel the human hallucinogenic data. These findings are consistent with evidence that 2,4,5- and 3,4,5-substituted phenylalkylamine hallucinogens exhibit distinct structure-activity relationships. These results provide additional evidence that the HTR assay can be used to investigate the structure-activity relationships of serotonergic hallucinogens.
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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.