In parkinsonism, glutamate pathways within the basal ganglia become overactive, leading to the suggestion that glutamate antagonists might possess antiparkinsonian qualities. This report examines the motor properties of antagonists of NMDA and AMPA-type glutamate receptors, as well as some inhibitors of glutamate release, in animal models of idiopathic Parkinson's disease. High affinity NMDA open-channel blockers (e.g. MK 801, phencyclidine), are highly potent antagonists with inconsistent antiakinetic and strong myorelaxant activity. Other compounds are better tolerated and are capable of relieving immobility and muscular rigidity by themselves (e.g. 1-aminoadamantanes, polyamine site antagonists, kappa agonists, riluzole). Yet others do not restore movements alone (e.g. dextromethorphan, ketamine), but may interact with and strengthen the antiparkinsonian action of L-DOPA (e.g. competitive NMDA and AMPA antagonists, lamotrigine). They may do this by potentiating dopaminergic behaviours mediated by D1 or D2 receptors, or by some other mechanism.

译文

在帕金森病中,基底神经节内的谷氨酸途径变得过度活跃,从而提示谷氨酸拮抗剂可能具有抗帕金森病的特性。该报告检查了特发性帕金森氏病动物模型中NMDA和AMPA型谷氨酸受体的拮抗剂的运动特性,以及谷氨酸释放的某些抑制剂。高亲和力NMDA开放通道阻滞剂(例如MK 801,苯环利定)是高效抗药,具有抗运动活性不一致和强肌松活性。其他化合物具有更好的耐受性,并能自行缓解不动和肌肉僵硬(例如1-氨基金刚烷,多胺位点拮抗剂,κ激动剂,利鲁唑)。还有一些人不能单独恢复运动(例如右美沙芬,氯胺酮),而是可以与L-DOPA相互作用并增强其抗帕金森病作用(例如竞争性NMDA和AMPA拮抗剂,拉莫三嗪)。他们可以通过增强D1或D2受体或其他某种机制介导的多巴胺能行为来做到这一点。

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