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_{2 A}), 2B (5-HT_{2 B}), and (5-HT_{2 C}) 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.

Keywords: 2C-E (2; 5-Dimethoxy-4-ethylphenethylamine); novel psychoactive substances (NPS); phenylethylamines; psychedelic; psychostimulants.

FIGURE 1

Time course of changes from baseline for physiological effects [°, 6.5–10 mg of 2C-E (n = 7), □, 15–25 mg of 2C-E (n = 3); mean, standard error].

FIGURE 2

Time course of changes from baseline for subjective effects [°, 6.5–10 mg of 2C-E (n = 7); □, 15–25 mg of 2C-E (n = 3); mean, standard error].

FIGURE 3

Time course of 2C-E concentrations in oral fluid [Δ, 6.5 mg of 2C-E (n = 1); °, 8–10 mg of 2C-E (n = 6), □, 15–25 mg of 2C-E (n = 3); mean, standard error].