McGovern Robin W, Middaugh Lawrence D, Patrick Kennerly S, Griffin William C
Center for Drug and Alcohol Programs, Medical University of South Carolina, Charleston, South Carolina 29425-0742, USA.
Behav Pharmacol. 2011 Feb;22(1):14-22. doi: 10.1097/FBP.0b013e3283423d92.
Methylphenidate (MPH) therapy for attention-deficit/hyperactivity disorder is common in children and adults. Concerns regarding abuse of MPH prompted studies to better understand its pharmacology. We used an established drug discrimination task to determine whether MPH could be discriminated by C57BL/6J (B6) mice. B6 mice learned to discriminate cues produced by racemic MPH (dl-MPH 5.0 mg/kg) or half the dose of pure d-isomer (2.5 mg/kg), and dose-response tests established appropriate reductions in discrimination with declining dose. Importantly, the two drug forms generalized to each other completely in substitution tests; consistent with reports that the l-isomer is pharmacodynamically inactive. An additional experiment indicated that lower doses (1 and 2 mg/kg) of dl-MPH did not support acquisition of MPH discrimination despite extensive training. Mice acquired discrimination of dl-MPH only when the dose was increased to 4 mg/kg. Thus, although these lower doses increased drug lever responding in mice trained on the higher dose, their stimuli were not sufficient to support acquisition of the discrimination task. These findings correspond to earlier studies conducted in our laboratory on threshold doses needed to produce stimulatory effects of motor activity in B6 mice. These preclinical findings provide insight into the relative potency, and by extension, efficacy of dl-MPH versus d-MPH doses.
哌甲酯(MPH)用于治疗儿童和成人的注意力缺陷多动障碍很常见。对MPH滥用的担忧促使开展研究以更好地了解其药理学特性。我们使用已确立的药物辨别任务来确定C57BL/6J(B6)小鼠是否能够辨别MPH。B6小鼠学会辨别消旋MPH(dl-MPH 5.0毫克/千克)或纯d-异构体一半剂量(2.5毫克/千克)产生的线索,剂量反应测试确定随着剂量降低辨别能力相应下降。重要的是,在替代测试中这两种药物形式能完全相互替代;这与l-异构体无药效学活性的报道一致。另一项实验表明,尽管经过广泛训练,较低剂量(1和2毫克/千克)的dl-MPH并不能支持小鼠习得MPH辨别能力。小鼠只有在剂量增加到4毫克/千克时才习得dl-MPH辨别能力。因此,尽管这些较低剂量增加了在较高剂量下训练的小鼠对药物杠杆的反应,但它们产生的刺激不足以支持习得辨别任务。这些发现与我们实验室早期关于在B6小鼠中产生运动活动刺激作用所需阈值剂量的研究结果一致。这些临床前研究结果有助于深入了解dl-MPH与d-MPH剂量的相对效力,进而了解其疗效。