Chloroquine, quinine and quinidine inhibit calcium release from macrophage intracellular stores by blocking inositol 1,4,5-trisphosphate binding to its receptor.

Published

Journal Article

The binding of many ligands to cellular receptors induces a signaling cascade which generates inositol 1,4,5-trisphosphate (IP3). IP3 binding to its receptors in various internal compartments causes a rapid Ca2+ efflux into the cytosol. We now demonstrate that chloroquine blocks ligand-induced Ca2+ mobilization without affecting IP3 synthesis. The effect is independent of the ligand employed and occurred with five unrelated ligands; namely, alpha 2-macroglobulin-methylamine, angiotensin II, bradykinin, carbachol, and epidermal growth factor. Chloroquine, quinidine, and quinine, however, block binding of [3H]IP3 to its receptors by 90%, 88%, and 71%, respectively. These observations suggest a previously undetected mechanism by which these agents may in part function as antimalarials.

Full Text

Duke Authors

Cited Authors

  • Misra, UK; Gawdi, G; Pizzo, SV

Published Date

  • February 1997

Published In

Volume / Issue

  • 64 / 2

Start / End Page

  • 225 - 232

PubMed ID

  • 9027583

Pubmed Central ID

  • 9027583

Electronic International Standard Serial Number (EISSN)

  • 1097-4644

International Standard Serial Number (ISSN)

  • 0730-2312

Digital Object Identifier (DOI)

  • 10.1002/(sici)1097-4644(199702)64:2<225::aid-jcb6>3.0.co;2-z

Language

  • eng