Loperamide: novel effects on capacitative calcium influx.

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Daly JW, Harper J

Loperamide: novel effects on capacitative calcium influx.

Cell Mol Life Sci. 2000 Jan 20;57(1):149-57.

PubMed ID

10949586 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Loperamide	Calmodulin	Protein	Humans	Unknown	Inhibitor	Details