Papaseit Esther, Farré Magí, Pérez-Mañá Clara, Torrens Marta, Ventura Mireia, Pujadas Mitona, de la Torre Rafael, González Débora
Clinical Pharmacology Unit, Germans Trias i Pujol University Hospital, Institute for Health Science Research Germans Trias i Pujol, Badalona, Spain.
Department of Pharmacology, Therapeutics and Toxicology and Department of Psychiatry and Forensic Medicine, Autonomous University of Barcelona, Barcelona, Spain.
Front Pharmacol. 2018 Mar 13;9:206. doi: 10.3389/fphar.2018.00206. eCollection 2018.
2,5-dimethoxy-4-bromophenethylamine (2C-B) is a psychedelic phenylethylamine derivative, structurally similar to mescaline. It is a serotonin 5-hydroxytryptamine-2A (5-HT), 5-hydroxytryptamine-2B (5-HT), and 5-hydroxytryptamine-2C (5-HT) 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.
2,5 - 二甲氧基 - 4 - 溴苯乙胺（2C - B）是一种致幻性苯乙胺衍生物，在结构上与三甲氧苯乙胺相似。它是一种血清素5 - 羟色胺 - 2A（5 - HT）、5 - 羟色胺 - 2B（5 - HT）和5 - 羟色胺 - 2C（5 - HT）受体部分激动剂，被作为一种新型精神活性物质用于娱乐。据报道，2C - B会诱发轻微的致幻效果，尽管其急性药理作用和药代动力学在人体中尚未得到充分研究。开展了一项观察性研究，以评估2C - B的急性主观和生理效应以及药代动力学。16名健康且有吸毒经验的使用者自行口服一剂2C - B（10、15或20毫克）。在基线以及1、2、3、4和6小时（h）测量生命体征（血压和心率）。每位参与者在基线、自行给药后2 - 3小时和6小时（6小时内的最大效应）以及致幻评定量表（6小时内的最大效应）使用三个评定量表完成主观效应评估：视觉模拟量表（VAS）、成瘾研究中心量表（ARCI）以及具有滥用潜力物质的主观效应评估量表（VESSPA - SSE）。收集口服液体（唾液）以评估24小时内的2C - B和皮质醇浓度。急性给予2C - B会使血压和心率升高。与欣快感相关的量表评分增加（兴奋、喜欢和刺激），并产生感知（距离、颜色、形状和光线）以及不同身体感觉/周围环境的变化。5名受试者描述有轻微的幻觉效应。自行给药后1小时和3小时分别达到2C - B和皮质醇的最大浓度。娱乐剂量的口服2C - B会诱发一系列类似于血清素作用药物的致幻/精神刺激样效应。
