Rao T S, Kim H S, Lehmann J, Martin L L, Wood P L
Research Department, Ciba-Geigy Pharmaceuticals Division, Summit, New Jersey.
J Neurochem. 1990 Apr;54(4):1157-62. doi: 10.1111/j.1471-4159.1990.tb01943.x.
Interactions of the potent phencyclidine receptor agonist MK-801 with the dopaminergic system were examined in various brain regions in the rat. MK-801 increased dopamine (DA) metabolism in the pyriform cortex, entorhinal cortex, prefrontal cortex, striatum, olfactory tubercle, amygdala, and septum without affecting DA metabolism in the cingulate cortex and nucleus accumbens. In pyriform cortex and amygdala, MK-801 was more potent than phencyclidine at increasing DA metabolism. Local injections of MK-801 into ventral tegmental area and into the amygdala/pyriform cortex interface indicated that MK-801 may act at the cell body as well as the nerve terminal level to increase DA metabolism and that ongoing dopaminergic neuronal activity is a prerequisite for full drug action.
在大鼠的不同脑区研究了强效苯环己哌啶受体激动剂MK-801与多巴胺能系统的相互作用。MK-801增加了梨状皮质、内嗅皮质、前额叶皮质、纹状体、嗅结节、杏仁核和隔区的多巴胺(DA)代谢,而不影响扣带皮质和伏隔核的DA代谢。在梨状皮质和杏仁核中,MK-801在增加DA代谢方面比苯环己哌啶更有效。向腹侧被盖区以及杏仁核/梨状皮质界面局部注射MK-801表明,MK-801可能在细胞体以及神经末梢水平起作用以增加DA代谢,并且持续的多巴胺能神经元活动是药物充分发挥作用的先决条件。