Lukomskaya N Y, Zhabko E P, Gmiro V E
I.M. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, St. Petersburg.
Neurosci Behav Physiol. 2000 Sep-Oct;30(5):543-6. doi: 10.1007/BF02462612.
The ability of the selective non-competitive NMDA receptor blocker MK-801 and a series of new glutamate antagonists --the adamantane derivatives IEM-1754 and IEM-1857 and phencyclidine (IEM-1925)--to prevent movement disorders induced by reversive rotation in mice was studied. l.p. MK-801 at a dose of 0.15 ml and IEM-1754 at a dose of 5.0 mg/kg prevented the development of akinesia in response to reversive rotation as effectively as scopolamine, a known agent which provides effective prophylaxis for movement diseases. IEM-1857, the quaternary analog of IEM-1754, was not effective. IEM-1925 significantly increased the responses of mice to reversive rotation, possibly because of its high activity in relation to other subtypes of glutamate receptors. These data provide evidence for the involvement of glutamatergic transmission in the mechanism of movement disorders of vestibular origin.
研究了选择性非竞争性N-甲基-D-天冬氨酸(NMDA)受体阻滞剂MK-801以及一系列新型谷氨酸拮抗剂——金刚烷衍生物IEM-1754和IEM-1857以及苯环利定(IEM-1925)预防小鼠反向旋转诱发的运动障碍的能力。腹腔注射剂量为0.15毫升的MK-801以及剂量为5.0毫克/千克的IEM-1754预防反向旋转引起的运动不能的效果与东莨菪碱一样有效,东莨菪碱是一种已知的能有效预防运动疾病的药物。IEM-1754的季铵类似物IEM-1857无效。IEM-1925显著增加了小鼠对反向旋转的反应,这可能是因为它对谷氨酸受体的其他亚型具有高活性。这些数据为谷氨酸能传递参与前庭源性运动障碍的机制提供了证据。