S Dethy, M A Laute, A Luxen, J Hildebrand, S Goldman
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引用次数: 6
摘要
我们采用自由活动大鼠纹间微透析模型,研究了培高利特对内源性和外源性左旋多巴生物转化的影响。培高利特是一种D1/D2多巴受体混合激动剂,在体内以D2受体为主。采用高效液相色谱法测定左旋多巴、DA、DOPAC、HVA和5-HIAA水平。培高利特(50 μ g /kg, i.p)使大鼠基底纹状体细胞外(EC) DOPAC、HVA和DA水平分别降低47%、65%和70%。卡比多巴后2小时注射L-DOPA (100 mg/kg, ig),局部灌注10(-4)M培高利特和未灌注10(-4)M培高利特大鼠L-DOPA、DOPAC、HVA和DA的EC水平显著升高。培高利特组DOPAC峰值较低,达到时间晚60分钟。本研究证实培高利特对内源性DA释放的抑制作用以及培高利特对外源性L-DOPA生物转化的影响。
Effect of pergolide on endogenous and exogenous L-DOPA metabolism in the rat striatum: a microdialysis study.
We used a model of intrastriatal microdialysis in freely moving rats to study the effect of pergolide, a mixed D1/D2 dopamine (DA) receptor agonist with predominant D2 action in vivo, on the biotransformation of endogenous and exogenous L-DOPA. Levels of L-DOPA, DA, DOPAC, HVA and 5-HIAA were measured by high performance liquid chromatography. Pergolide (50 micrograms/kg, i.p.) caused a 47%, 65% and 70% decrease in basal striatal extracellular (EC) levels of DOPAC, HVA and DA, respectively. L-DOPA (100 mg/kg, i.p.), injected 2 hours after carbidopa, produced significant increase in EC levels of L-DOPA, DOPAC, HVA and DA in rats with and without local perfusion of 10(-4) M pergolide. The DOPAC peak value was lower and was reached 60 minutes later in the group with pergolide. This study demonstrated inhibitory effects of pergolide on endogenous DA release and influence of pergolide on exogenous L-DOPA biotransformation.