Papaseit Esther, Olesti Eulalia, Pérez-Mañá Clara, Torrens Marta, Grifell Marc, Ventura Mireia, Pozo Oscar J, de Sousa Fernandes Perna Elizabeth B, Ramaekers Johannes G, de la Torre Rafael, Farré Magí
Clinical Pharmacology Unit, Hospital Universitari Germans Trias i Pujol-Institut de Recerca Germans Trias i Pujol (HUGTiP-IGTP), Badalona, Spain.
Department of Pharmacology, Therapeutics and Toxicology and Department of Psychiatry and Forensic Medicine, Universitat Autònoma de Barcelona (UAB), Barcelona, Spain.
Front Pharmacol. 2020 Mar 18;11:233. doi: 10.3389/fphar.2020.00233. eCollection 2020.
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 ), 2B (5-HT ), and (5-HT ) 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.
2,5-二甲氧基-4-乙苯乙胺(2C-E)是一种致幻苯乙胺,其化学结构与三甲氧苯乙胺相似,用作新型精神活性物质(NPS)。它抑制去甲肾上腺素和5-羟色胺的摄取,更重要的是,它作为5-羟色胺2A(5-HT₂A)、2B(5-HT₂B)和2C(5-HT₂C)受体的部分激动剂。消费者报告称,2C-E会引发轻度至中度的致幻效果,但其在人体中的药理学,包括药理作用和药代动力学,尚未得到研究。为了评估2C-E对生理和主观效应的急性影响,并评估其药代动力学,开展了一项观察性研究。10名迷幻剂的娱乐使用者自行口服单剂量的2C-E(6.5、8、10、15或25毫克)。在给药前、给药后2小时、4小时和6小时评估血压和心率。采用三个评定量表来评估主观效应:一组视觉模拟量表(VAS)、成瘾研究中心量表(ARCI)的49项简版以及具有滥用潜力物质主观效应评估量表(VESSPA-SSE),在自行给药前、给药后2小时、4小时和6小时进行评估。为了评估2C-E的浓度,在6小时内收集口服液体(唾液)。2C-E主要引起感知、幻觉和欣快感的改变。自行给药后2小时唾液浓度达到最大值。以娱乐剂量口服2C-E会产生一组类似于2C-B和其他5-羟色胺作用药物的致幻样效应。