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哌甲酯在C57BL/6J小鼠中的辨别性刺激特性。

The discriminative stimulus properties of methylphenidate in C57BL/6J mice.

作者信息

McGovern Robin W, Middaugh Lawrence D, Patrick Kennerly S, Griffin William C

机构信息

Center for Drug and Alcohol Programs, Medical University of South Carolina, Charleston, South Carolina 29425-0742, USA.

出版信息

Behav Pharmacol. 2011 Feb;22(1):14-22. doi: 10.1097/FBP.0b013e3283423d92.

DOI:10.1097/FBP.0b013e3283423d92
PMID:21160424
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3099148/
Abstract

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.

摘要

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。

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Transdermal and oral dl-methylphenidate-ethanol interactions in C57BL/6J mice: transesterification to ethylphenidate and elevation of d-methylphenidate concentrations.C57BL/6J 小鼠经皮和口服 dl-哌甲酯-乙醇相互作用:转酯化生成乙基哌甲酯和 d-哌甲酯浓度升高。
J Pharm Sci. 2011 Jul;100(7):2966-78. doi: 10.1002/jps.22476. Epub 2011 Jan 14.

本文引用的文献

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J Pharmacol Exp Ther. 2010 Jun;333(3):834-43. doi: 10.1124/jpet.110.165746. Epub 2010 Feb 26.
2
The interactive effects of methylphenidate and ethanol on ethanol consumption and locomotor activity in mice.哌醋甲酯和乙醇对小鼠乙醇摄入量和运动活性的交互作用。
Pharmacol Biochem Behav. 2010 May;95(3):267-72. doi: 10.1016/j.pbb.2010.01.009. Epub 2010 Feb 1.
3
Reinforcing and subjective effects of methylphenidate in adults with and without attention deficit hyperactivity disorder (ADHD).哌甲酯对患有和未患有注意力缺陷多动障碍(ADHD)的成年人的强化作用和主观效应。
Psychopharmacology (Berl). 2009 May;204(1):73-83. doi: 10.1007/s00213-008-1439-6. Epub 2008 Dec 23.
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Evolution of stimulants to treat ADHD: transdermal methylphenidate.治疗注意力缺陷多动障碍(ADHD)的兴奋剂的演变:透皮哌甲酯。
Hum Psychopharmacol. 2009 Jan;24(1):1-17. doi: 10.1002/hup.992.
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Safety of therapeutic methylphenidate in adults: a systematic review of the evidence.成人使用治疗性哌甲酯的安全性:证据的系统评价
J Psychopharmacol. 2009 Mar;23(2):194-205. doi: 10.1177/0269881108089809. Epub 2008 May 30.
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