Carlsson M, Svensson A
Department of Pharmacology, University of Göteborg, Sweden.
Pharmacol Biochem Behav. 1990 May;36(1):45-50. doi: 10.1016/0091-3057(90)90123-y.
In the present paper it is shown that when either of the noncompetitive NMDA antagonists MK-801 or ketamine are combined with the alpha-adrenergic agonist clonidine, a pronounced stimulation of locomotion is produced in monoamine-depleted mice. Likewise, when a subthreshold dose of MK-801 is combined with the muscarinic antagonist atropine, a forceful synergism with regard to locomotor activity in monoamine-depleted mice is observed. Furthermore, the present study shows that also in monoamine-depleted rats MK-801, as well as the competitive NMDA antagonist AP-5 (DL-2-amino-5-phosphonovaleric acid), interact synergistically with clonidine to enhance locomotor activity. Taken together, our findings suggest that central glutamatergic systems exert a powerful inhibitory influence on locomotion. Interfering with this inhibitory force by administration of an NMDA antagonist promotes locomotion and discloses the activational potential of other transmitter systems. The results are discussed in relation to 1) the pathophysiology of schizophrenia, with emphasis on the glutamate hypothesis of schizophrenia, and 2) implications for the treatment of Parkinson's disease.
本文表明,当非竞争性NMDA拮抗剂MK-801或氯胺酮与α-肾上腺素能激动剂可乐定联合使用时,单胺耗竭的小鼠会出现明显的运动兴奋。同样,当亚阈剂量的MK-801与毒蕈碱拮抗剂阿托品联合使用时,在单胺耗竭的小鼠中观察到对运动活动有强烈的协同作用。此外,本研究表明,在单胺耗竭的大鼠中,MK-801以及竞争性NMDA拮抗剂AP-5(DL-2-氨基-5-磷酸戊酸)与可乐定协同作用以增强运动活动。综上所述,我们的研究结果表明,中枢谷氨酸能系统对运动施加强大的抑制作用。通过给予NMDA拮抗剂干扰这种抑制力可促进运动,并揭示其他递质系统的激活潜力。将对结果进行如下讨论:1)精神分裂症的病理生理学,重点是精神分裂症的谷氨酸假说;2)对帕金森病治疗的意义。