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3,4-二氯苯丙烯酰异丁胺(7903)抗实验性癫痫的机制分析

ANALYSIS OF THE MECHANISM OF ANTICONVULSANT ACTION OF 3,4-DICHLOROPHENYL PROPENYL ISOBUTYLAMIDE (7903)

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【作者】 曹龙光裴印权

【Author】 CAO Long-guang and PEI Yin-quan (Department of Pharmacology, Beijing Medical College)

【机构】 北京医学院药理教研组北京医学院药理教研组

【摘要】 本实验初步分析了7903抗小鼠MES的作用机制。这种作用可能与其影响脑内5-HT的代谢有关;因为7903使脑内5-HT含量升高的时间变化规律与其抗小鼠MES效应的时间规律有密切的相关性。此外,用利血平降低脑内单胺类介质时,可使7903抗MES作用明显减弱。单独使用PCPA减少脑内5-HT含量时,也减弱7903的抗MES作用。相反,给利血平化的小鼠单独补充5-HT前体L-色氨酸,提高脑内5-HT含量则可加强7903的抗MES作用。可见,7903的抗MES作用与5-HT的功能有关。

【Abstract】 The mechanism of anticonvulsant action of 7903 was studied. It may be related to serotoninergic system. 7903 was found to be able to increase the concentration of 5-HT and 5-HIAA in mice brain. The peak time of such action was at the first hour after treatment and gradually returned to normal level within 12 hours. This change of 5-HT was closely related to its anticonvulsant action, the correlation coefficent was 0.93 (P<0.001). Results of other experiments further support this finding. Reserpine was shown to antagonize the anticonvulsant action of 7903. Reserpinized mice were pretreated with L-tryptophane, the precursor of 5-HT, to supplement the concentration of depleted 5-HT (nearly to 80%).In such a condition, the anticonvulsant action of 7903 was recovered. In contrast, normal mice pretreated with PCPA to block the synthesis of 5-HT, decreased the anticonvulsant action of 7903.The concentration of NE was slightly decreased at the first hour after treatment with 7903, then gradually increased, and reached a peak on the 12th hours after treatment. At this time, the anticonvulsant action of the drug completely disappeared. The concentration of DA did not change within the 12-hour period.

  • 【文献出处】 药学学报 ,Acta Pharmaceutica Sinica , 编辑部邮箱 ,1982年12期
  • 【被引频次】6
  • 【下载频次】38
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