Fang J, Yu P H
Department of Psychiatry, University of Saskatchewan, Saskatoon, Canada.
Neuropharmacology. 1994 Jun;33(6):763-8. doi: 10.1016/0028-3908(94)90116-3.
The effect on dopamine uptake by L-deprenyl, its structural analogues and different types of monoamine oxidase (MAO) inhibitors was investigated. Both direct [3H]dopamine uptake into rat striatal slices and binding of a specific dopamine uptake inhibitor [3H]GBR-12935 were used in the present study. L-Deprenyl exhibits a relatively weak dopamine uptake inhibitory effect in vitro, while D-deprenyl possesses a very potent inhibitory effect. The potent effect of D-deprenyl on dopamine uptake may be responsible, at least in part, for its behavioral effects and abuse liability. L-Methamphetamine, a metabolite of L-deprenyl, does not inhibit [3H]GBR-12935 binding but it reduces the retention of [3H]dopamine in striatal tissues, suggesting that it may enhance dopamine release. The MAO-A inhibitors clorgyline and brofaromine also exhibit dopamine uptake inhibitory effects. Irreversible and reversible MAO-B inhibitors, however, such as pargyline, aliphatic N-methylpropargylamines, Ro 19-6327 and MDL-72974A and MAO-A inhibitor moclobemide do not possess any appreciable inhibitory effects on dopamine uptake. Dopamine uptake is probably unrelated to the pharmacological actions of L-deprenyl.
研究了L-司来吉兰、其结构类似物以及不同类型的单胺氧化酶（MAO）抑制剂对多巴胺摄取的影响。本研究采用了将[3H]多巴胺直接摄取到大鼠纹状体切片以及特异性多巴胺摄取抑制剂[3H]GBR-12935的结合这两种方法。L-司来吉兰在体外表现出相对较弱的多巴胺摄取抑制作用，而D-司来吉兰具有非常强的抑制作用。D-司来吉兰对多巴胺摄取的强效作用可能至少部分地解释了其行为效应和滥用倾向。L-司来吉兰的代谢产物L-甲基苯丙胺不抑制[3H]GBR-12935的结合，但它会降低纹状体组织中[3H]多巴胺的保留量，这表明它可能会增强多巴胺的释放。MAO-A抑制剂氯吉兰和溴法罗明也表现出多巴胺摄取抑制作用。然而，不可逆和可逆的MAO-B抑制剂，如帕吉林、脂肪族N-甲基炔丙胺、Ro 19-6327和MDL-72974A以及MAO-A抑制剂吗氯贝胺对多巴胺摄取没有任何明显的抑制作用。多巴胺摄取可能与L-司来吉兰的药理作用无关。
