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GABAB受体介导对小鼠额叶皮质中内源性5-羟色胺钾诱发释放的抑制作用。

GABAB-receptor mediated inhibition of potassium-evoked release of endogenous 5-hydroxytryptamine from mouse frontal cortex.

作者信息

Gray J A, Green A R

出版信息

Br J Pharmacol. 1987 Jul;91(3):517-22. doi: 10.1111/j.1476-5381.1987.tb11244.x.

DOI:10.1111/j.1476-5381.1987.tb11244.x
PMID:3038240
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1853550/
Abstract

The effect of baclofen, the GABAB-agent, on the potassium-evoked release of endogenous 5-hydroxytryptamine (5-HT) from slices of mouse frontal cortex has been investigated. The release of endogenous 5-HT evoked by addition of K+ (35 mM) was inhibited by (+/-)-baclofen in a dose-dependent manner with an IC50 of 0.1 microM. Inhibition of K+-evoked release of 5-HT was produced by (+/-)- and (-)-baclofen but not (+)-baclofen. This action of the (-)-enantiomer was not altered by the presence of the (+)-enantiomer. Addition of GABA (0.1-10 microM) also induced a dose-dependent inhibition of 5-HT release. This effect was neither enhanced by flurazepam (1 microM) nor antagonized by bicuculline (10 microM). The progabide metabolite, 4-[( (4-chlorophenyl) (5-fluoro-2-hydroxyphenyl)methylene]amino)butyric acid (SL75.102) (1 microM) inhibited the K+-evoked release of 5-HT by 61%. These data suggest that baclofen is a potent inhibitor of the K+-evoked release of endogenous 5-HT from the cortex and further indicate that the release of 5-HT may be controlled by a GABAB-receptor located presynaptically.

摘要

已研究了γ-氨基丁酸B（GABAB）受体激动剂巴氯芬对小鼠额叶皮质切片中钾离子诱发的内源性5-羟色胺（5-HT）释放的影响。添加K+（35 mM）诱发的内源性5-HT释放受到（±）-巴氯芬的剂量依赖性抑制，半数抑制浓度（IC50）为0.1μM。（±）-和（-）-巴氯芬可抑制钾离子诱发的5-HT释放，但（+）-巴氯芬则无此作用。（-）-对映体的这一作用不受（+）-对映体存在的影响。添加γ-氨基丁酸（GABA，0.1 - 10μM）也可诱导5-HT释放的剂量依赖性抑制。氟西泮（1μM）既不增强此效应，荷包牡丹碱（10μM）也不拮抗此效应。普罗加比的代谢产物4-[（（4-氯苯基）（5-氟-2-羟基苯基）亚甲基]氨基丁酸（SL75.102）（1μM）可使钾离子诱发的5-HT释放抑制61%。这些数据表明，巴氯芬是皮质中钾离子诱发的内源性5-HT释放的有效抑制剂，并进一步表明5-HT的释放可能受突触前GABAB受体的调控。

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本文引用的文献

1
Protein measurement with the Folin phenol reagent.使用福林酚试剂进行蛋白质测定。
J Biol Chem. 1951 Nov;193(1):265-75.
2
Inhibitory GABAergic influence on striatal serotonergic transmission exerted in the dorsal raphe as revealed by in vivo voltammetry.体内伏安法揭示了背侧中缝核中抑制性γ-氨基丁酸能对纹状体5-羟色胺能传递的影响。
Brain Res. 1984 Jul 9;305(2):343-52. doi: 10.1016/0006-8993(84)90440-2.
3
gamma-Aminobutyric acid (GABA) receptor stimulation. I. Neuropharmacological profiles of progabide (SL 76002) and SL 75102, with emphasis on their anticonvulsant spectra.γ-氨基丁酸（GABA）受体刺激作用。I. 普罗加比（SL 76002）和SL 75102的神经药理学特征，重点在于其抗惊厥谱。
J Pharmacol Exp Ther. 1982 Mar;220(3):660-71.
4
GABAB receptor-mediated inhibition of serotonin release in the rat brain.大鼠脑中GABAB受体介导的5-羟色胺释放抑制作用
Naunyn Schmiedebergs Arch Pharmacol. 1984 Jun;326(2):99-105. doi: 10.1007/BF00517304.
5
gamma-Aminobutyric acid (GABA) receptor stimulation. II. Specificity of progabide (SL 76002) and SL 75102 for the GABA receptor.γ-氨基丁酸（GABA）受体刺激作用。II. 普罗加比（SL 76002）和SL 75102对GABA受体的特异性。
J Pharmacol Exp Ther. 1982 Mar;220(3):672-7.
6
Differences between the release of radiolabelled and endogenous dopamine from superfused rat brain slices: effects of depolarizing stimuli, amphetamine and synthesis inhibition.从超灌流大鼠脑片中释放的放射性标记多巴胺与内源性多巴胺之间的差异：去极化刺激、苯丙胺及合成抑制的影响
Brain Res. 1985 Dec 2;348(2):309-20. doi: 10.1016/0006-8993(85)90450-0.
7
Precise determination of 5-hydroxytryptamine in platelets and platelet-poor plasma.血小板及乏血小板血浆中5-羟色胺的精确测定。
Clin Chem. 1985 Sep;31(9):1573-4.
8
Comparison of the action of baclofen with gamma-aminobutyric acid on rat hippocampal pyramidal cells in vitro.巴氯芬与γ-氨基丁酸对大鼠海马锥体细胞体外作用的比较。
J Physiol. 1985 Mar;360:161-85. doi: 10.1113/jphysiol.1985.sp015610.
9
The effects of the GABA-mimetic drugs, progabide and baclofen, on the biochemistry and function of 5-hydroxytryptamine and noradrenaline.γ-氨基丁酸模拟药物普罗加比和巴氯芬对5-羟色胺和去甲肾上腺素的生物化学及功能的影响。
Neuropharmacology. 1986 Jul;25(7):711-6. doi: 10.1016/0028-3908(86)90086-9.
10
Changes in gamma-aminobutyric acid biochemistry and seizure threshold.
Ann N Y Acad Sci. 1986;462:105-19. doi: 10.1111/j.1749-6632.1986.tb51245.x.

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