INC Research, Toronto, Ontario, Canada.
J Clin Psychopharmacol. 2012 Aug;32(4):492-502. doi: 10.1097/JCP.0b013e31825d380d.
Taranabant is a cannabinoid 1 receptor inverse agonist that was in development for treatment of obesity. Because of central nervous system effects, the study was performed to assess the abuse potential and cognitive effects of taranabant in recreational polydrug users compared with phentermine, dronabinol, and placebo.
Stimulant- and cannabis-experienced polydrug users (N = 30) were randomized in a double-blind crossover study to receive taranabant 2, 4, 10, and 20 mg; phentermine 45 and 90 mg; dronabinol 20 mg; and placebo. Subjective and neurocognitive measures were administered for 24 hours, and peak/peak change from baseline effects were analyzed using a linear mixed-effects model.
Phentermine 45 and 90 mg showed abuse-related subjective effects versus placebo, including drug liking, overall drug liking, and other positive/stimulant effects, whereas dronabinol 20 mg showed abuse-related positive, cannabis-like, and sedative effects. Taranabant was not significantly different from placebo on most of the subjective measures other than negative/dysphoric effects at the highest dose, and its effects were significantly less pronounced relative to phentermine and dronabinol on most measures. Phentermine improved cognitive/motor performance and dronabinol impaired motor/cognitive performance on some measures, whereas taranabant 4 and 20 mg had minor impairment effects on manual tracking.
The phentermine and dronabinol results demonstrate the validity and sensitivity of the study. Taranabant did not consistently show stimulant/cannabis-like effects or abuse potential in recreational polydrug users, indicating that cannabinoid 1 receptor inverse agonists/antagonists are unlikely to be recreationally abused.
Taranabant 是一种大麻素 1 受体反向激动剂,用于治疗肥胖症。由于其对中枢神经系统的影响,进行了这项研究以评估与安非他命相比,在娱乐性多药使用者中 taranabant 的滥用潜力和认知效应,大麻隆和安慰剂。
经验丰富的兴奋剂和大麻的多药使用者(N = 30)被随机分为双盲交叉研究,接受 taranabant 2、4、10 和 20 mg;安非他命 45 和 90 mg;大麻隆 20 mg;和安慰剂。在 24 小时内进行主观和神经认知测量,并使用线性混合效应模型分析从基线变化的峰值/峰值效应。
安非他命 45 和 90 mg 与安慰剂相比显示出与滥用相关的主观效应,包括药物喜好、总体药物喜好和其他积极/兴奋剂效应,而大麻隆 20 mg 显示出与滥用相关的积极、大麻样和镇静效应。除了最高剂量的负面/烦躁效应外,与安慰剂相比,Taranabant 在大多数主观测量中没有显著差异,并且相对于安非他命和大麻隆,其作用在大多数测量中明显较轻。安非他命改善了认知/运动表现,而大麻隆在某些测量中损害了运动/认知表现,而 taranabant 4 和 20 mg 在手动跟踪方面仅有轻微的损害作用。
安非他命和大麻隆的结果证明了研究的有效性和敏感性。在娱乐性多药使用者中,Taranabant 并未一致显示出兴奋剂/大麻样效应或滥用潜力,这表明大麻素 1 受体反向激动剂/拮抗剂不太可能被滥用。