Göthert M, Fink K
Institut für Pharmakologie und Toxikologie, Rheinischen Friedrich-Wilhelms-Universität Bonn, Federal Republic of Germany.
Naunyn Schmiedebergs Arch Pharmacol. 1989 Nov;340(5):516-21. doi: 10.1007/BF00260606.
The influence of ethanol on stimulation-evoked 3H-transmitter release was examined in slices of the rat brain cortex and corpus striatum preincubated with 3H-noradrenaline and 3H-choline, respectively. 3H-Transmitter release was stimulated by NMDA, L-glutamate, electrical impulses, reintroduction of Ca2+ ions ("Ca2(+)-evoked release", after superfusion with Ca2(+)-free, K(+)-rich solution) or veratridine. In cortical slices preincubated with 3H-noradrenaline and superfused with Mg2(+)-free, otherwise physiologically composed salt solution, ethanol inhibited the NMDA- or L-glutamate-induced tritium overflow (IC50 45 and 37 mmol/l, respectively). In contrast, the tritium overflow in response to electrical stimulation, reintroduction of Ca2+ ions or veratridine was not affected by ethanol at concentrations up to 320 mmol/l; these experiments were carried out in cortical slices superfused with solution containing a physiological Mg2+ concentration. Ethanol also failed to inhibit Ca2(+)-evoked release in the absence of Mg2+ ions. In the presence of 1 mumol/l veratridine, but not in its absence, NMDA induced tritium overflow even when cortical slices were superfused with salt solution containing a physiological Mg2+ concentration; again, ethanol inhibited this NMDA-evoked tritium overflow (IC50 73 mmol/l. In striatal slices preincubated with 3H-choline and superfused with Mg2(+)-free "physiological" salt solution the NMDA-evoked tritium overflow was also, although at lower potency, inhibited by ethanol (IC50 192 mmol/l). In spite of the differences between the IC50 values of ethanol determined for the inhibition of cortical noradrenaline and striatal acetylcholine release, it may be concluded that the NMDA receptor-ion channel complex is one of the sites of action underlying the ethanol-induced inhibition of neurotransmitter release.(ABSTRACT TRUNCATED AT 250 WORDS)
分别用3H-去甲肾上腺素和3H-胆碱预孵育大鼠大脑皮层和纹状体切片,研究乙醇对刺激诱发的3H递质释放的影响。3H递质释放通过N-甲基-D-天冬氨酸(NMDA)、L-谷氨酸、电冲动、重新引入Ca2+离子(在无Ca2+、富含K+的溶液灌注后出现的“Ca2+诱发释放”)或藜芦碱来刺激。在用3H-去甲肾上腺素预孵育并灌注无Mg2+、其他成分与生理盐溶液相同的溶液的皮层切片中,乙醇抑制NMDA或L-谷氨酸诱导的氚溢出(IC50分别为45和37 mmol/L)。相反,在灌注含生理Mg2+浓度溶液的皮层切片中,浓度高达320 mmol/L的乙醇对电刺激、重新引入Ca2+离子或藜芦碱所引起的氚溢出没有影响;这些实验是在这样的皮层切片中进行的。在无Mg2+离子的情况下,乙醇也不能抑制Ca2+诱发的释放。在存在1 μmol/L藜芦碱时,即使皮层切片灌注含生理Mg2+浓度的盐溶液,NMDA也会诱导氚溢出;同样,乙醇抑制这种NMDA诱发的氚溢出(IC50为73 mmol/L)。在用3H-胆碱预孵育并灌注无Mg2+的“生理”盐溶液的纹状体切片中,NMDA诱发的氚溢出也受到乙醇抑制(尽管效力较低,IC50为192 mmol/L)。尽管测定乙醇抑制皮层去甲肾上腺素和纹状体乙酰胆碱释放的IC50值存在差异,但可以得出结论,NMDA受体-离子通道复合物是乙醇诱导神经递质释放抑制作用的作用位点之一。(摘要截短于250词)