Molina V A, Orsingher O A
Arch Int Pharmacodyn Ther. 1981 May;251(1):66-79.
Acute or repeated treatment with Mg-Pemoline (Mg-Pg) did not modify the endogenous level of brain catecholamines (CA) of rats. However, a single dose (30 mg/kg) produced a significant decrease of brain CA turnover, measured either by the rate of conversion of 14C-tyrosine to CA or by the rate of disappearance of CA after alpha-MT. Mg-Pe (0.01-0.1 mM) did not modify the basal outflow nor the release of 3H-DA elicited by high K+ in slices of corpus striatum. At the same concentrations, Mg-Pe inhibited uptake of DA (competitively) or NA (uncompetitively) in synaptosomes from corpus striatum and hypothalamus, respectively. Turning-behavior in mice lesioned in corpus striatum with 6-OH-DA, indicated that this drug acts like amphetamine as an indirect DA agonist. These results suggest that central stimulant effects of Mg-Pe may be the consequence of CA-uptake inhibition and this effect may also account for the decrease of brain CA turnover.
用匹莫林镁（Mg-Pg）进行急性或重复治疗，并未改变大鼠脑内儿茶酚胺（CA）的内源性水平。然而，单次给药（30毫克/千克）会使脑内CA周转率显著降低，这一降低通过14C-酪氨酸向CA的转化速率或α-甲基酪氨酸（alpha-MT）处理后CA的消失速率来衡量。匹莫林乙酯（Mg-Pe，0.01 - 0.1毫摩尔）既不改变纹状体切片中基础递质释放量，也不改变高钾引发的3H-多巴胺（3H-DA）释放量。在相同浓度下，匹莫林乙酯分别竞争性抑制纹状体突触体中多巴胺（DA）的摄取以及非竞争性抑制下丘脑突触体中去甲肾上腺素（NA）的摄取。用6-羟基多巴胺（6-OH-DA）损伤纹状体的小鼠的旋转行为表明，该药物作为间接DA激动剂，其作用类似于苯丙胺。这些结果表明，匹莫林乙酯的中枢兴奋作用可能是CA摄取抑制的结果，并且这种作用也可能是脑内CA周转率降低的原因。
