INVIVO EFFECTS OF SUMATRIPTAN (GR-43175) ON EXTRACELLULAR LEVELS OF 5-HT IN THE GUINEA-PIG

被引:70
作者
SLEIGHT, AJ [1 ]
CERVENKA, A [1 ]
PEROUTKA, SJ [1 ]
机构
[1] STANFORD UNIV,MED CTR,DEPT NEUROL,STANFORD,CA 94305
关键词
5-HT release; 5-HT terminal autoreceptor; 5-HT[!sub]ID[!/sub] receptors; intracerebral dialysis;
D O I
10.1016/0028-3908(90)90061-U
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
The effect of sumatriptan, a selective 5-HTID receptor agent, on extracellular levels of 5-HT in the frontal cortex of the guinea pig was measured by intracerebral dialysis. A constant infusion of sumatriptan (10-8-10-7 M) dose-dependently reduced extracellular levels of 5-HT (e.g. 80 ± 2% decrease from control levels of 5-HT at 10-7 M). Peripheral administration of sumatriptan (50 μg/kg i.p. and 500 μg/kg i.p.) had no effect on extracellular levels of 5-HT in the frontal cortex. These data suggest that sumatriptan, when infused into the brain, inhibits the release of 5-HT by stimulating 5-HT autoreceptors and that the putative acute anti-migraine effects of sumatriptan are likely to be mediated by peripheral mechanisms. © 1990.
引用
收藏
页码:511 / 513
页数:3
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