Comparison of the behavioral and biochemical effects of the NMDA receptor antagonists, MK-801 and phencyclidine.
Comparison of the behavioral and biochemical effects of the NMDA receptor antagonists, MK-801 and phencyclidine.
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NMDA 受体拮抗剂 MK-801 和苯环己哌啶的行为和生化效应的比较。
DOI：
10.1016/0014-2999(89)90346-4
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发表时间：
1989
影响因子：
5
通讯作者：
Nabeshima,T
中科院分区：
文献类型：
--
作者：
Hiramatsu,M;Cho,AK;Nabeshima,T
本文比较了非竞争性N-甲基-D-天冬氨酸（NMDA）受体拮抗剂MK-801（（+）-5-甲基-10，11-二氢-5H-二苯并[a，d]环庚烯-5，10-亚胺马来酸盐）与苯环己哌啶（PCP）的行为学和生化作用。在本研究中使用的剂量范围内，MK-801（0.125 - 0.5 mg/kg i.p.）产生共济失调和其他行为反应，与五氯苯酚（5 - 10 mg/kg i.p.）相似。然而，MK-801诱导的转向和后退不具有剂量依赖性，并且在产生与PCP大致相同水平的共济失调的剂量下强度较低。神经化学上，MK-801（0.5mg/kg i.p.）增加皮层和纹状体多巴胺的周转，但对5-HT系统无影响。它抑制5-HT摄取的效力也比五氯苯酚低3.4倍。这些结果表明，MK-801诱导的行为反应主要涉及PCP受体和多巴胺系统，与PCP的差异反映了对5-HT神经元系统的影响降低。
The behavioral and biochemical effects of the noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist, MK-801 ((+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine maleate) were compared with those of phencyclidine (PCP). In the dose range used in this study, MK-801 (0.125-0.5 mg/kg i.p.) produced ataxia and other behavioral responses which were similar to PCP (5–10 mg/kg i.p.). However, turning and backpedalling induced by MK-801 were not dose-dependent and less intense at the dose producing approximately the same level of ataxia as PCP. Neurochemically, MK-801 (0.5 mg/kg i.p.) increased dopamine turnover in the cortex and striatum, but had no effect on 5-HT system. It was also 3.4 times less potent in inhibiting 5-HT uptake than PCP. These results suggest that the behavioral responses induced by MK-801 involve primarily the PCP receptor and the dopamine system, and that the differences from PCP reflect a reduced effect on the 5-HT neuronal system.