米帕林对完整和透化大鼠胰腺腺泡淀粉酶分泌的抑制作用。

Inhibition by mepacrine and amylase secretion from intact and permeabilized rat pancreatic acini.

作者信息

Grosfils K, Gomez F, Dehaye J P

机构信息

Department of General and Human Biochemistry, Free University of Brussels, Belgium.

出版信息

Biochem Biophys Res Commun. 1992 Apr 15;184(1):408-13. doi: 10.1016/0006-291x(92)91208-8.

DOI:10.1016/0006-291x(92)91208-8

PMID:1373616

Abstract

In intact rat pancreatic acini, the phospholipase A2 inhibitor mepacrine did not affect basal amylase release but dose-dependently inhibited the carbachol (IC50 65 microM) and CCK-8 (IC50 210 microM)-stimulated amylase release. In permeabilized acini, mepacrine shifted the dose-response curve for calcium to the right by a factor 2 and inhibited the release of amylase stimulated by GTPrS. From these results we conclude that carbachol, CCK-8 and GTPrS probably activate a phospholipase A2 closely coupled to exocytosis.

摘要

在完整的大鼠胰腺腺泡中，磷脂酶A2抑制剂米帕林不影响基础淀粉酶释放，但剂量依赖性地抑制卡巴胆碱（IC50为65微摩尔）和八肽胆囊收缩素（CCK-8，IC50为210微摩尔）刺激的淀粉酶释放。在通透化腺泡中，米帕林使钙的剂量反应曲线右移2倍，并抑制了由鸟苷-5'-O-（3-硫代三磷酸）（GTPrS）刺激的淀粉酶释放。从这些结果我们得出结论，卡巴胆碱、CCK-8和GTPrS可能激活了一种与胞吐作用紧密偶联的磷脂酶A2。