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格列本脲及其结构类似物HB 699对ob/ob小鼠胰岛45Ca2+摄取的不同影响。

Different effects of glibenclamide and the structural analogue HB 699 on the 45Ca2+ uptake by ob/ob-mouse islets.

作者信息

Norlund L, Sehlin J

出版信息

Acta Physiol Scand. 1984 Oct;122(2):187-90. doi: 10.1111/j.1748-1716.1984.tb07497.x.

Abstract

The effects on 45Ca2+ uptake of HB 699, an acyl-amino-alkyl benzoic acid derivative, was compared to those of glibenclamide in incubations using the La3+ wash technique. HB 699 enhanced the 45Ca2+ net uptake in a concentration range (10-200 microM) where insulin release was also stimulated. Glibenclamide showed maximum stimulation of 45Ca2+ net uptake already at 1 microM. HB 699 did not clearly stimulate the short-term 45Ca2+ uptake whether or not the islets were preincubated with the drug. It is suggested that HB 699-induced insulin release is mediated, at least partly, by increased mobility of beta-cell Ca2+.

摘要

使用镧离子洗脱技术进行孵育,比较了酰基氨基烷基苯甲酸衍生物HB 699和格列本脲对45Ca2+摄取的影响。在刺激胰岛素释放的浓度范围(10-200微摩尔)内,HB 699增强了45Ca2+的净摄取。格列本脲在1微摩尔时就显示出对45Ca2+净摄取的最大刺激作用。无论胰岛是否预先用该药物孵育,HB 699均未明显刺激短期45Ca2+摄取。提示HB 699诱导的胰岛素释放至少部分是由β细胞Ca2+流动性增加介导的。

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