Loperamide: novel effects on capacitative calcium influx

被引：21

作者：

Daly, JW ^{[1
]}

Harper, J ^{[1
]}

机构：

[1] Natl Inst Hlth, Bioorgan Chem Lab, Bethesda, MD 20892 USA

来源：

CELLULAR AND MOLECULAR LIFE SCIENCES | 2000年 / 57卷 / 01期

关键词：

loperamide; calcium channels; calcium stores; maitotoxin; inositol trisphosphate; thapsigargin; ATP;

D O I：

10.1007/s000180050504

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Loperamide is a widely used antidiarrheal that primarily acts at nanomolar concentrations through activation of opioid receptors in the gastrointestinal tract. At somewhat higher concentrations, loperamide blocks calmodulin activity, calcium channels, N-methyl-D-aspartate-receptor channels, and maitotoxin-elicited calcium influx. Loperamide at micromolar concentrations has now been shown to have a remarkable stimulatory effect on the capacitative calcium influx that is triggered in many cells by depletion of the inositol-trisphosphate-sensitive stores of calcium in the endoplasmic reticulum. The mechanism whereby loperamide enhances levels of intracellular calcium elevated by capacitative calcium influx is, as yet, undefined.

引用

页码：149 / 157

页数：9

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