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钙激动剂和拮抗剂对小脑颗粒细胞的作用。

Effect of calcium agonists and antagonists on cerebellar granule cells.

作者信息

Kingsbury A, Balazs R

机构信息

Medical Research Council, Developmental Neurobiology Unit, London, U.K.

出版信息

Eur J Pharmacol. 1987 Aug 21;140(3):275-83. doi: 10.1016/0014-2999(87)90284-6.

Abstract

In cerebellar cultures, comprising predominantly granule neurones, dihydropyridine (DHP) Ca2+ agonists were potent stimulators of voltage-sensitive 45Ca2+ uptake. Their effect was maximal in partially depolarized cells; at 15 mM K+e half maximal stimulation occurred at about 5 X 10(-8) M BAY K 8644 and 10(-7) M (+)-(S)-202791. Organic Ca2+ antagonists were effective inhibitors of voltage-sensitive calcium entry into granule cells: the order of potency in blocking uptake induced by sub-maximal concentration of K+ and BAY K 8644 was nifedipine greater than (-)-202791 greater than D600. BAY K 8644 also stimulated the release of glutamate, the transmitter of the granule cells, from depolarized cells. Granule cells are therefore a class of neurones whose responsiveness to organic Ca2+ effectors is similar to that of cardiac and smooth muscle. The discrepant findings on the effect of calcium effectors in various preparations of nervous tissues may thus reflect a differential distribution of voltage-sensitive Ca2+ channels in different neuronal cell types.

摘要

在主要由颗粒神经元组成的小脑培养物中,二氢吡啶(DHP)钙激动剂是电压敏感性45Ca2+摄取的有效刺激剂。它们的作用在部分去极化细胞中最大;在15 mM K+e时,约5×10(-8) M BAY K 8644和10(-7) M (+)-(S)-202791时出现半数最大刺激。有机钙拮抗剂是电压敏感性钙进入颗粒细胞的有效抑制剂:在阻断由次最大浓度的K+和BAY K 8644诱导的摄取方面,效力顺序为硝苯地平大于(-)-202791大于D600。BAY K 8644还刺激颗粒细胞的递质谷氨酸从去极化细胞中释放。因此,颗粒细胞是一类神经元,其对有机钙效应器的反应性与心肌和平滑肌相似。神经组织各种制剂中钙效应器作用的差异结果可能因此反映了电压敏感性钙通道在不同神经元细胞类型中的差异分布。

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