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苯甲曲秦、氨基苯唑和对氯苯丙胺对脑儿茶酚胺类物质的运动活性及更新率的影响。

Effect of phenmetrazine, aminorex and ( ) p-chloramphetamine on the motor activity and turnover rate of brain catecholamines.

作者信息

Costa E, Naimzada K M, Revuelta A

出版信息

Br J Pharmacol. 1971 Nov;43(3):570-9. doi: 10.1111/j.1476-5381.1971.tb07187.x.

Abstract
  1. The minimal doses (mumol/kg i.v.) of phenmetrazine, (+/-)-p-chloramphetamine, and aminorex which increase motor activity are 5.6, 3.5, and 1.5, respectively. We detected stereotype behaviour neither in rats receiving intravenous doses 3 times greater nor in animals injected intraperitoneally with 44, 62 and 112 mumol/kg of (+/-)-p-chloramphetamine, aminorex and phenmatrazine, respectively.2. The latter doses of the three amphetamine congeners were tested for their action on tissue monoamine content. Only (+/-)-p-chloramphetamine decreased the concentration of tel-diencephalon 5-hydroxytryptamine (5-HT) and this decrease lasted longer than 24 hours. This and the other two amphetamine congeners failed to affect the concentration of noradrenaline (NA) in brain, heart and lung.3. Aminorex (1.5 mumol/kg i.v.) and (+/-)-p-chloramphetamine (3.5 mumol/kg i.v.) decreased the turnover time of striatum dopamine (DM) but failed to change the turnover time of tel-diencephalon and brainstem NA. Phenmetrazine (5.6 mumol/kg i.v.) changed neither the turnover time of striatum DM nor that of NA in the two brain areas assayed.
摘要
  1. 能够增加运动活性的苯甲曲秦、(±)-对氯苯丙胺和氨基苯唑的最小剂量(微摩尔/千克静脉注射)分别为5.6、3.5和1.5。我们在接受3倍以上静脉剂量的大鼠中,以及分别腹腔注射44、62和112微摩尔/千克(±)-对氯苯丙胺、氨基苯唑和苯甲曲秦的动物中均未检测到刻板行为。

  2. 对这三种苯丙胺同系物的后一组剂量测试了它们对组织单胺含量的作用。只有(±)-对氯苯丙胺降低了终脑-间脑5-羟色胺(5-HT)的浓度,且这种降低持续超过24小时。这三种苯丙胺同系物中的这一种以及另外两种均未影响脑、心脏和肺中去甲肾上腺素(NA)的浓度。

  3. 氨基苯唑(1.5微摩尔/千克静脉注射)和(±)-对氯苯丙胺(3.5微摩尔/千克静脉注射)缩短了纹状体多巴胺(DM)的周转时间,但未改变终脑-间脑和脑干NA的周转时间。苯甲曲秦(5.6微摩尔/千克静脉注射)在检测的两个脑区中既未改变纹状体DM的周转时间,也未改变NA的周转时间。

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本文引用的文献

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LOWERING OF BRAIN SEROTONIN LEVEL BY CHLORAMPHETAMINES.氯苯丙胺降低脑血清素水平
Biochem Pharmacol. 1965 Apr;14:483-8. doi: 10.1016/0006-2952(65)90221-2.

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