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钙通道拮抗剂维拉帕米和加洛帕米是分离和富集的豚鼠壁细胞中酸分泌的强力抑制剂。

Calcium channel antagonists verapamil and gallopamil are powerful inhibitors of acid secretion in isolated and enriched guinea pig parietal cells.

作者信息

Sewing K F, Hannemann H

出版信息

Pharmacology. 1983;27(1):9-14. doi: 10.1159/000137824.

Abstract

In isolated and enriched guinea pig parietal cells the inhibitory effects of the calcium channel antagonists verapamil and gallopamil on 14C-aminopyrine uptake (= H+ secretion) have been analyzed. Both verapamil and gallopamil inhibit acid secretion in a concentration-dependent manner with an IC50 of 12.1 and 10.9 mumol/l respectively. The type of inhibition is noncompetitive in nature. Verapamil inhibits the acid response to histamine, dibutyryl-cAMP, and KCl with IC50 values not significantly different from each other. Exposure of the cells to verapamil and subsequent washing enhances the acid response to histamine for an unknown reason. It is concluded that the calcium channel antagonists verapamil and gallopamil inhibit acid secretion in vitro by interfering with the parietal cell proton pump, the K+/H+-ATPase.

摘要

在分离和富集的豚鼠壁细胞中,已分析了钙通道拮抗剂维拉帕米和加洛帕米对14C-氨基比林摄取(=H+分泌)的抑制作用。维拉帕米和加洛帕米均以浓度依赖性方式抑制酸分泌,IC50分别为12.1和10.9μmol/L。抑制类型本质上是非竞争性的。维拉帕米抑制对组胺、二丁酰环磷腺苷和氯化钾的酸反应,其IC50值彼此无显著差异。将细胞暴露于维拉帕米并随后洗涤,由于未知原因增强了对组胺的酸反应。结论是,钙通道拮抗剂维拉帕米和加洛帕米通过干扰壁细胞质子泵(K+/H+-ATP酶)在体外抑制酸分泌。

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