Poyatos Lourdes, Pérez-Mañá Clara, Hladun Olga, Núñez-Montero Melani, de la Rosa Georgina, Martín Soraya, Barriocanal Ana Maria, Carabias Lydia, Kelmendi Benjamin, Taoussi Omayema, Busardò Francesco Paolo, Fonseca Francina, Torrens Marta, Pichini Simona, Farré Magí, Papaseit Esther
Department of Clinical Pharmacology, Hospital Universitari Germans Trias i Pujol and Institut de Recerca Germans Trias i Pujol (HUGTiP-IGTP), Badalona, Spain.
Department of Pharmacology, Therapeutics and Toxicology, Universitat Autònoma de Barcelona (UAB), Cerdanyola del Vallés, Spain.
Front Pharmacol. 2023 Feb 17;14:1122861. doi: 10.3389/fphar.2023.1122861. eCollection 2023.
Methylone is one of the most common synthetic cathinones popularized as a substitute for 3,4-methylenedioxymethamphetamine (MDMA, midomafetamine) owing to its similar effects among users. Both psychostimulants exhibit similar chemistry (i.e., methylone is a β-keto analog of MDMA) and mechanisms of action. Currently, the pharmacology of methylone remains scarcely explored in humans. Herein, we aimed to evaluate the acute pharmacological effects of methylone and its abuse potential in humans when compared with that of MDMA following oral administration under controlled conditions. Seventeen participants of both sexes (14 males, 3 females) with a previous history of psychostimulant use completed a randomized, double-blind, placebo-controlled, crossover clinical trial. Participants received a single oral dose of 200 mg of methylone, 100 mg of MDMA, and a placebo. The variables included physiological effects (blood pressure, heart rate, oral temperature, pupil diameter), subjective effects using visual analog scales (VAS), the short form of the Addiction Research Center Inventory (ARCI), the Evaluation of Subjective Effects of Substances with Abuse Potential questionnaire (VESSPA-SSE), and the Sensitivity to Drug Reinforcement Questionnaire (SDRQ), and psychomotor performance (Maddox wing, psychomotor vigilance task). We observed that methylone could significantly increase blood pressure and heart rate and induce pleasurable effects, such as stimulation, euphoria, wellbeing, enhanced empathy, and altered perception. Methylone exhibited an effect profile similar to MDMA, with a faster overall onset and earlier disappearance of subjective effects. These results suggest that abuse potential of methylone is comparable to that of MDMA in humans. https://clinicaltrials.gov/ct2/show/NCT05488171; Identifier: NCT05488171.
甲酮是最常见的合成卡西酮之一，因其在使用者中产生的效果相似，被推广用作3,4-亚甲基二氧甲基苯丙胺（摇头丸，米多非他明）的替代品。这两种精神兴奋剂具有相似的化学性质（即甲酮是摇头丸的β-酮类似物）和作用机制。目前，甲酮在人体中的药理学研究仍很少。在此，我们旨在评估在受控条件下口服给药后，甲酮的急性药理作用及其在人体中的滥用潜力，并与摇头丸进行比较。17名有精神兴奋剂使用史的参与者（14名男性，3名女性）完成了一项随机、双盲、安慰剂对照、交叉临床试验。参与者分别单次口服200毫克甲酮、100毫克摇头丸和安慰剂。变量包括生理效应（血压、心率、口腔温度、瞳孔直径）、使用视觉模拟量表（VAS）的主观效应、成瘾研究中心量表简版（ARCI）、具有滥用潜力物质主观效应评估问卷（VESSPA-SSE）和药物强化敏感性问卷（SDRQ），以及精神运动表现（马多克斯翼试验、精神运动警觉任务）。我们观察到，甲酮可显著升高血压和心率，并产生愉悦效应，如刺激、欣快感、幸福感、增强的同理心和感知改变。甲酮的效应特征与摇头丸相似，主观效应的总体起效更快且消失更早。这些结果表明，甲酮在人体中的滥用潜力与摇头丸相当。https://clinicaltrials.gov/ct2/show/NCT05488171；标识符：NCT05488171。
