Psychopharmacology
March 1, 2014
Amy J Eshleman, Michael J Forster, Katherine M Wolfrum et al.
72 citations
Six substituted phenethylamines (2C-C, 2C-D, 2C-E, 2C-I, 2C-T-2, and DOC) depress mouse locomotor activity, though 2C-D and 2C-E stimulate activity at low doses. Most fully substitute for hallucinogenic training compounds in rats, but none fully substitute for methamphetamine. All are full agonists at 5-HT2A and 5-HT2C receptors in inositol phosphate assays, and most are partial to full agonists in 5-HT2A arachidonic acid release assays, except 2C-I (antagonist). Only 2C-I shows moderate affinity for the serotonin transporter. The discriminative stimulus effects of most compounds resemble hallucinogens, not methamphetamine, but 2C-T-2 does not produce hallucinogen-like effects despite being a full agonist at 5-HT2A and 5-HT2C receptors.
Frontiers in pharmacology
January 1, 2026
Michael B Gatch, Shuping Jia, Ritu A Shetty et al.
Two synthetic cathinones found on the street, N-cyclohexyl butylone and N-cyclohexyl methylone, were tested for their psychostimulant effects in mice and rats. Both compounds stimulated locomotor activity in mice, but were less potent and less effective than methamphetamine. In rats trained to discriminate methamphetamine or cocaine from saline, N-cyclohexyl butylone fully substituted for those drugs, suggesting it could produce similar psychoactive effects and motivate illicit use. N-cyclohexyl methylone failed to fully substitute for methamphetamine or cocaine and caused convulsions at higher doses, indicating greater danger but possibly lower abuse liability. Neither compound substituted for MDMA. The large N-cyclohexyl chemical group likely reduced the drugs' effectiveness, but a longer side chain in N-cyclohexyl butylone may have counteracted this.
Journal of psychopharmacology (Oxford, England)
April 4, 2025
Rebecca D Hill, Ritu A Shetty, Nathalie Sumien et al.
Three new synthetic tryptamines—5-MeO-DBT, 5-Cl-DMT, and 4-OH-MiPT—were tested in mice and rats for their effects on movement and their ability to mimic the hallucinogen DOM. All three produced depressant phases similar to DOM but were less potent. In rats trained to discriminate DOM, only 4-OH-MiPT fully substituted for DOM, suggesting it shares DOM's abuse potential, while 5-MeO-DBT and 5-Cl-DMT did not fully substitute and decreased response rates.
bioRxiv : the preprint server for biology
February 17, 2025
Rajiv S Rangan, R Max Petty, Suchismita Acharya et al.
preprint
Psychedelics can produce lasting changes in brain function beyond their immediate mind-altering effects, which is being explored for treating mental health disorders. The authors propose that psychedelics may modify proteins by covalently attaching to them through a process called transamidation, mediated by transglutaminase enzymes. They synthesized a modified version of mescaline, a psychedelic phenethylamine from cacti, and used click-chemistry in human astrocyte cell cultures to identify potential protein targets. Preliminary results suggest many glial proteins could be substrates for this modification, which they term phenethylaminylation. This speculative mechanism may help explain long-term cognitive changes from single psychedelic doses.