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

Abstract

2,5-dimethoxy-4-bromophenethylamine (2C-B) is a psychedelic phenylethylamine derivative, structurally similar to mescaline. It is a serotonin 5-hydroxytryptamine-2A (5-HT2A), 5-hydroxytryptamine-2B (5-HT2B), and 5-hydroxytryptamine-2C (5-HT2C) receptor partial agonist used recreationally as a new psychoactive substance. It has been reported that 2C-B induces mild psychedelic effects, although its acute pharmacological effects and pharmacokinetics have not yet been fully studied in humans. An observational study was conducted to assess the acute subjective and physiological effects, as well as pharmacokinetics of 2C-B. Sixteen healthy, experienced drug users self-administered an oral dose of 2C-B (10, 15, or 20 mg). Vital signs (blood pressure and heart rate) were measured at baseline 1, 2, 3, 4, and 6 hours (h). Each participant completed subjective effects using three rating scales: the visual analog scale (VAS), the Addiction Research Centre Inventory (ARCI), and the Evaluation of the Subjective Effects of Substances with Abuse Potential (VESSPA-SSE) at baseline, 2–3 and 6 h after self-administration (maximum effects along 6 h), and the Hallucinogenic Rating Scale (maximum effects along 6 h). Oral fluid (saliva) was collected to assess 2C-B and cortisol concentrations during 24 h. Acute administration of 2C-B increased blood pressure and heart rate. Scores of scales related to euphoria increased (high, liking, and stimulated), and changes in perceptions (distances, colors, shapes, and lights) and different body feelings/surrounding were produced. Mild hallucinating effects were described in five subjects. Maximum concentrations of 2C-B and cortisol were reached at 1 and 3 h after self-administration, respectively. Oral 2C-B at recreational doses induces a constellation of psychedelic/psychostimulant-like effects similar to those associated with serotonin-acting drugs.

A qualitative descriptive analysis of effects of psychedelic phenethylamines and tryptamines

“…Many users described entactogenic effects similar to MDMA. We believe that these descriptions add to previous literature that notes that 2C‐B use is associated with euphoria and mild hallucinations (Gonzalez, Torrens, & Farre, ; Papaseit et al, ). The use of other 2C series compounds was less common, and the effects have not been described in great detail in the published literature.…”

Population Survey Data Informing the Therapeutic Potential of Classic and Novel Phenethylamine, Tryptamine, and Lysergamide Psychedelics

“…These pharmacological outcomes, predicted to occur more frequently with phenethylamine (and especially the novel 2C phenethylamine) drugs than tryptamines, could underlie the observed associations of these novel phenethylamines with negative psychological health. In support of this view, 2C-B, the most commonly reported novel phenethylamine, is often substituted for MDMA among electronic music party goers secondary to its purported psychostimulant properties (15,20,65). Indeed, novel phenethylamines are often described in terms of psychostimulant effects (20,29), whereas challenging, emotional breakthrough, and mystical-type experiences appear to underlie the therapeutic outcomes of the classic tryptamine psychedelic psilocybin (16,66,67).…”

“…In support of this view, 2C-B, the most commonly reported novel phenethylamine, is often substituted for MDMA among electronic music party goers secondary to its purported psychostimulant properties (15,20,65). Indeed, novel phenethylamines are often described in terms of psychostimulant effects (20,29), whereas challenging, emotional breakthrough, and mystical-type experiences appear to underlie the therapeutic outcomes of the classic tryptamine psychedelic psilocybin (16,66,67). Thus, with regard to acute subjective effects, it may be that novel phenethylamines are characterized more so by problematic psychostimulant outcomes and less so by salubrious challenging, emotional breakthrough, and mystical-type experiences.…”

“…5-HT2A receptor agonism), they differ in chemical structure, which appears to account for differences in reported subjective effects (19). It is known that psychedelics interact differently with their target 5-HT 2A receptor (20). That is to say, they engage with different sets of amino acid residues in the binding pocket of the receptor to produce slightly different active state conformations of the receptor.…”

LC‐MS/MS method for the quantification of new psychoactive substances and evaluation of their urinary detection in humans for doping control analysis

“…The volunteers were asked to report their stimulant effect at baseline, 1, 2, and 4 h post drug administration through the measurement of the stimulation feeling rate at that precise moment via visual analog scales (VAS: 100 mm, from “not at all” to “extremely”) …”