Kendle Early Stage-Toronto, Ontario, Canada.
Clin Pharmacol Ther. 2010 Jul;88(1):69-78. doi: 10.1038/clpt.2010.67. Epub 2010 Jun 2.
Tesofensine is a (triple) reuptake inhibitor of noradrenaline, dopamine, and serotonin that is in development for the treatment of obesity. The abuse potential of triple reuptake inhibitors is not yet known, and so this study was undertaken to evaluate the potential abuse-related effects of tesofensine in humans. It was designed as a single-dose, randomized, double-blind, crossover study involving tesofensine vs. placebo, D-amphetamine (positive control for dopaminergic/stimulant effects), bupropion, and atomoxetine (negative/unscheduled controls) in recreational stimulant users (N = 52). Subjective and objective measures were assessed for 48 h after drug administration. The study results show that the effects of D-amphetamine were significantly greater than those of placebo on all primary and secondary subjective measures. The effects of tesofensine were not significantly different from those of placebo and were lower than those of D-amphetamine 30 mg on all primary and most secondary measures. The effects of tesofensine were either lower than or not different from those of bupropion or atomoxetine. These results demonstrate that the abuse potential for tesofensine is no greater than that of bupropion or atomoxetine, and tesofensine is therefore unlikely to be recreationally abused.
特索芬辛是一种去甲肾上腺素、多巴胺和 5-羟色胺的（三重）再摄取抑制剂，目前正在开发用于治疗肥胖症。三重再摄取抑制剂的滥用潜力尚不清楚，因此进行了这项研究，以评估特索芬辛在人类中的潜在滥用相关作用。这是一项单剂量、随机、双盲、交叉研究，涉及特索芬辛与安慰剂、D-苯丙胺（多巴胺/兴奋剂作用的阳性对照）、安非他酮和托莫西汀（阴性/非计划对照），在娱乐性兴奋剂使用者中（N=52）。给药后 48 小时评估主观和客观测量。研究结果表明，D-苯丙胺的作用明显大于安慰剂在所有主要和次要主观测量。特索芬辛的作用与安慰剂无显著差异，且在所有主要和大多数次要测量中，30 毫克 D-苯丙胺的作用均低于特索芬辛。特索芬辛的作用低于或与安非他酮或托莫西汀的作用无差异。这些结果表明，特索芬辛的滥用潜力不大于安非他酮或托莫西汀，因此特索芬辛不太可能被滥用。
