The administration of numerous facilitatory drugs in combination with appropriate physiotherapeutic approaches is reported to facilitate neurorehabilitation. First evidence of the possible beneficial influence of facilitatory drugs in neurorehabilitation arose from studies investigating the pharmacology of learning in healthy humans. Amphetamine, for example, has shown to improve performance of different somatosensory and motor skills. Paired with physical therapy in stroke patients, it also increases the rate and extent of motor recovery and supports treatment of aphasia. Amphetamine is however known as a "dirty drug", because it acts non-specifically by increasing centrally the levels of dopamine, serotonin, and noradrenaline. Thus, first approaches intend to scrutinize the role of more specifically acting pharmacological agents on learning and neurorehabilitation. In this review, focus is placed on two main topics: (i) studies that aimed to investigate the pharmacological basis of motor and sensory skills in healthy humans and (ii) studies investigating whether the same drugs may also support neurorehabilitation. First, different sensorimotor paradigms are discussed, which were introduced to investigate basic influences of facilitatory pharmaceuticals on cortical plasticity. Then, emphasis is placed on the role of these drugs acting to gate synaptic plasticity in neurorehabilitation. It is concluded that further studies in large populations should focus on more specifically acting pharmaceuticals, their side effects and their capacity in supporting different patterns of physical therapy.