METOCLOPRAMIDE AND SULPIRIDE AS SELECTIVE BLOCKING-AGENTS OF PRESYNAPTIC AND POSTSYNAPTIC DOPAMINE-RECEPTORS
METOCLOPRAMIDE AND SULPIRIDE AS SELECTIVE BLOCKING-AGENTS OF PRESYNAPTIC AND POSTSYNAPTIC DOPAMINE-RECEPTORS
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DOI：
10.1007/bf00569723
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发表时间：
1980-01-01
影响因子：
3.6
通讯作者：
GRABOWSKAANDEN, M
中科院分区：
文献类型：
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作者：
ALANDER, T;ANDEN, NE;GRABOWSKAANDEN, M
舒必利和甲氧氯普胺对突触前和突触后多巴胺受体的影响进行了研究，在大鼠大脑中，作为阿扑吗啡诱导的多巴胺合成抑制的拮抗作用，在没有神经冲动的情况下，作为阻断阿扑吗啡诱导的旋转后，单侧失活的纹状体，分别。舒必利对突触后多巴胺受体的阻断作用强于突触前多巴胺受体，而甲氧氯普胺则相反。舒必利和甲氧氯普胺可促进多巴胺的合成和利用，阿托品、哌唑嗪和氨氧乙酸可抑制多巴胺的合成和利用。3种药物的抑制作用均能被胃复安所抵消，而舒必利则不能。这种差异可以用甲氧氯普胺对突触前多巴胺受体的优先作用来解释。单侧纹状体失活后，低剂量的甲氧氯普胺（而不是舒必利）使大鼠同侧翻转，表明多巴胺的释放被促进，突触前多巴胺受体具有生理意义。
The effects of sulpiride and metoclopramide on pre- and postsynaptic dopamine receptors were investigated in the rat brain as antagonism of the apomorphine-induced inhibition of the dopamine synthesis in the absence of nerve impulses and as blockade of the as blockade of the apomorphine-induced rotation following unilateral inactivation of the corpus striatum, respectively. Sulpiride was more potent in blocking post- than presynaptic dopamine receptors but the reverse was found for metoclopramide. The synthesis and the utilization of dopamine was stimulated by sulpiride and metaclopramide and was inhibited by atropine, prazosin and aminooxyacetic acid. The inhibitory effects of the 3 drugs were counteracted by metoclopramide, but not by sulpiride. This difference can be explained by the preferential action of metoclopramide on presynaptic dopamine receptors. Following unilateral inactivation of the corpus striatum, metoclopramide at a low dose, but not sulpiride turned the rats ipsilaterally, indicating that the release of dopamine was facilitated and that the presynaptic dopamine receptors are of physiological significance.