Gramsbergen Jan Bert, Cumming Paul
Anatomy & Neurobiology, Institute of Medical Biology, University of Southern Denmark, Winsløwparken 21, DK-5000 Odense C, Denmark.
Neurochem Int. 2007 Jul;51(1):8-15. doi: 10.1016/j.neuint.2007.03.004. Epub 2007 Mar 18.
The pathway for selective serotonergic toxicity of 3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") is poorly understood, but has been linked to hyperthermia and disturbed energy metabolism. We investigated the dose-dependency and time-course of MDMA-induced perturbations of cerebral glucose metabolism in freely moving rats using rapid sampling microdialysis (every minute) coupled to flow-injection analysis (FIA) with biosensors for glucose and lactate. Blood samples for analysis of glucose and lactate were taken at 30-45 min intervals before and after drug dosing and body temperature was monitored by telemetry. A single dose of MDMA (2-10-20 mg/kg i.v.) evoked a transient increase of interstitial glucose concentrations in striatum (139-223%) with rapid onset and of less than 2h duration, a concomitant but more prolonged lactate increase (>187%) at the highest MDMA dose and no significant depletions of striatal serotonin. Blood glucose and lactate levels were also transiently elevated (163 and 135%) at the highest MDMA doses. The blood glucose rises were significantly related to brain glucose and brain lactate changes. The metabolic perturbations in striatum and the hyperthermic response (+1.1 degrees C) following systemic MDMA treatment were entirely blocked in p-chlorophenylalanine pre-treated rats, indicating that these effects are mediated by endogenous serotonin.
3,4-亚甲基二氧甲基苯丙胺(摇头丸,MDMA)的选择性5-羟色胺能毒性途径目前了解甚少,但已被认为与体温过高及能量代谢紊乱有关。我们利用快速采样微透析技术(每分钟一次),结合用于葡萄糖和乳酸盐的生物传感器进行流动注射分析(FIA),对自由活动的大鼠中MDMA诱导的脑葡萄糖代谢紊乱的剂量依赖性和时间进程进行了研究。在给药前和给药后,每隔30 - 45分钟采集血样以分析葡萄糖和乳酸盐,并通过遥测监测体温。静脉注射单剂量MDMA(2 - 10 - 20毫克/千克)可使纹状体间质葡萄糖浓度短暂升高(139 - 223%),起效迅速且持续时间不到2小时,在最高MDMA剂量时伴随有更持久的乳酸盐升高(>187%),而纹状体5-羟色胺无显著消耗。在最高MDMA剂量时,血糖和血乳酸水平也短暂升高(分别为163%和135%)。血糖升高与脑葡萄糖及脑乳酸变化显著相关。在对氯苯丙氨酸预处理的大鼠中,全身给予MDMA后的纹状体代谢紊乱及体温升高反应(+1.1摄氏度)完全被阻断,这表明这些效应是由内源性5-羟色胺介导的。