Acute Effects of 2C-E in Humans: An Observational Study

Abstract

2,5-Dimethoxy-4-ethylphenethylamine (2C-E) is psychedelic phenylethylamine, with a chemical structure similar to mescaline, used as new psychoactive substance (NPS). It inhibits norepinephrine and serotonin uptake and, more relevant, acts as a partial agonist of the serotonin 2A (5-HT 2A ), 2B (5-HT 2B ), and (5-HT 2C ) receptors. Consumers have reported that 2C-E induces mild-moderate psychedelic effects, but its pharmacology in humans, including pharmacological effects and pharmacokinetics, have not yet studied. To assess the acute effects of 2C-E on physiological and subjective effects and evaluate its pharmacokinetics, an observational study was carried-out. Ten recreational users of psychedelics self-administered a single oral dose of 2C-E (6.5, 8, 10, 15, or 25 mg). Blood pressure and heart rate were evaluated at baseline, 2, 4, and 6 h post-administration. Three rating scales were administered to evaluate subjective effects: a set of Visual Analog Scales (VAS), the 49-item short form version of the Addiction Research Centre Inventory (ARCI), and the Evaluation of the Subjective Effects of Substances with Abuse Potential (VESSPA-SSE) at baseline, 2, 4, and 6 h after self-administration. To assess 2C-E concentrations oral fluid (saliva) was collected during 6 h. 2C-E induced primarily alterations in perceptions, hallucinations, and euphoric-mood. Saliva maximal concentrations were achieved 2 h after self-administration. Administration of oral 2C-E at recreational doses produces a group of psychedelic-like effects such to 2C-B and other serotonin-acting drugs.

Acute Pharmacological Effects of Oral and Intranasal Mephedrone: An Observational Study in Humans

“…The study was conducted according to a non-controlled prospective observational study with minimal intervention in subjects who self-administered mephedrone orally or intranasally. Similarly to previous naturalistic observational studies evaluating acute effects of other NPS, the methodology including evaluations and procedures were similar [ 39 , 40 ]. Each subject participated in one session.…”

“…Subjective effects of mephedrone were measured at baseline and at 1, 2, and 4 h after self-administration using different scales and questionnaires. A set of Visual Analog Scales (VAS) (100 mm, from “not at all” to “extremely”) were used to measure rate intensity; stimulated; high; good effects; liking; content; changes in colors; changes in shapes; changes in lights; hallucinations—seeing of lights or spots; hallucinations—seeing animals, things, insects, or people; changes in hearing; hallucinations—hearing sounds or voices; different body feeling; unreal body feeling; changes in distances; different surroundings; unreal surroundings; confusion; fear; depression or sadness; drowsiness; dizziness; bad effects; headache; nausea; vertigo; breathing difficulty; and face flushing [ 29 , 39 , 40 , 41 , 42 ]. The 49-item Addiction Research Centre Inventory (ARCI) short form, a validated instrument that includes subscales related to drug sedation (pentobarbital chlorpromazine-alcohol group, PCAG), euphoria (morphine-benzedrine group, MBG), dysphoria and somatic symptoms (lysergic acid diethylamide group, LSD), intellectual efficiency and energy (benzedrine group, BG), and d-amphetamine like effects (A) that evaluate subjective effects produced by psychoactive drugs [ 38 , 39 ].…”

“…After collection, samples were centrifuged and frozen at −20 °C until analysis. Mephedrone concentrations were analyzed by a validated LC-MS/MS [ 39 , 40 ]. A Mephedrone chromatogram (one participant that self-administrated orally 150 mg of mephedrone and one participant that self-administrated 50 mg intranasal) and chromatograms of the internal standard used for the previous samples (Mephedrone-d3) were available in Supplementary Figure S2 and linearity parameters of the oral fluid methodology in Supplementary Figure S3 .…”

Acute Pharmacological Effects and Oral Fluid Biomarkers of the Synthetic Cannabinoid UR-144 and THC in Recreational Users

“…Subjective effects were measured with visual analogue scales (VAS), the 49-item Addiction Research Center Inventory form (ARCI) and the Evaluation of Subjective Effects of Substances with Abuse Potential questionnaire (VESSPA). A set of different VAS [100 mm (mm)] labeled with different adjectives marked at opposite ends with “not at all” and “extremely” were employed [ 24 , 25 ]. Subjects were asked to rate effects such as “intensity”, “high”, “good effects”, “bad effects”, “hunger”, “drowsiness”, “dizziness”, “confusion”, “nausea”, “vomits”, “anxiety”, “aggressiveness”, “hallucinations-seeing of lights or spots”, “hallucinations-hearing sounds or voices” and “hallucinations-seeing animals, things, insects or people”.…”

A Comparison of Acute Pharmacological Effects of Methylone and MDMA Administration in Humans and Oral Fluid Concentrations as Biomarkers of Exposure

“…The study was designed as a non-controlled prospective observational study in a naturalistic setting with methylone and MDMA self-administration. The methodology, including procedures and evaluations, coincides with previous observational–naturalistic studies aimed at evaluating the acute effects of other NPS [ 38 , 39 , 40 ]. Six subjects (5 M, 1 F) self-administered MDMA and 8 subjects (5 M, 3 F) self-administered methylone.…”