Kannari K, Markstein R
Preclinical Research, Sandoz Pharma, Basle, Switzerland.
J Neural Transm Gen Sect. 1991;84(3):211-20. doi: 10.1007/BF01244971.
The competitive NMDA-antagonists SDZ EAA-494 and CGP 37849 and the mixed D-1/D-2 dopamine agonists CI 201-678 and SDZ 205-152 reverse akinesia in monoamine-depleted mice in a dose dependent manner. Combination of threshold doses of NMDA-antagonists with dopamine agonists markedly enhances anti-akinetic effects. CI 201-678 which in addition to D-1 and D-2 receptors stimulates alpha-2 receptors produces a stronger effect than SDZ 205-152 which is devoid of alpha-2 agonist activity. The results indicate that concomitant blockade of NMDA-receptors and activation of dopamine receptors results in synergistic or at least additive motor stimulatory effects.
竞争性N-甲基-D-天冬氨酸(NMDA)拮抗剂SDZ EAA-494和CGP 37849,以及混合性D-1/D-2多巴胺激动剂CI 201-678和SDZ 205-152能以剂量依赖性方式逆转单胺耗竭小鼠的运动不能。NMDA拮抗剂的阈剂量与多巴胺激动剂联合使用可显著增强抗运动不能作用。除了D-1和D-2受体外还刺激α-2受体的CI 201-678比缺乏α-2激动剂活性的SDZ 205-152产生更强的作用。结果表明,同时阻断NMDA受体和激活多巴胺受体可产生协同或至少相加的运动刺激作用。