Methylphenidate (MPH) is currently the most widely used molecule in the pharmacologic treatment of attention-deficit hyperactivity disorder (ADHD). Although experience of its application now extends over several decades, its psychotropic nature, prolonged use in children, and chemical relation to amphetamines still raise doubts in the minds of prescribers and the families of the patients. Brain imaging has shed considerable light on the neuropharmacology of MPH. The two main in vivo neuroimaging techniques are positron-emission tomography (PET) and magnetic resonance imaging (MRI), and these can be applied in both animal models and humans. The present review seeks to show how human molecular and functional imaging has contributed to determining not only the molecular targets of MPH, and the action kinetics of the various pharmaceutical forms available, but also the connectivity and brain networks activated by treatment. We also discuss the perspectives opened up by new hybrid PET–MRI techniques that enable multimodal tracking of the impact of methylphenidate on neurotransmission.

哌醋甲酯（MPH）是目前在注意力缺陷多动障碍（ADHD）药物治疗中使用最广泛的分子。尽管其应用经验已经扩展了几十年，但其精神性质，在儿童中的长期使用以及与苯丙胺的化学关系仍然在开药者和患者家属的心中引起怀疑。大脑成像已为MPH的神经药理学提供了可观的启示。体内的两个主要神经成像技术是正电子发射断层扫描（PET）和磁共振成像（MRI），这些技术可以应用于动物模型和人类。本综述旨在显示人类分子和功能成像如何不仅有助于确定MPH的分子靶标，可利用的各种药物形式的作用动力学，而且还有助于确定由治疗激活的连接性和大脑网络。我们还将讨论新的PET-MRI混合技术所带来的前景，这些技术能够对哌醋甲酯对神经传递的影响进行多峰跟踪。