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

Publication ,  Journal Article
Misra, UK; Gawdi, G; Pizzo, SV
Published in: J Cell Biochem
February 1997

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.

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Published In

J Cell Biochem

DOI

ISSN

0730-2312

Publication Date

February 1997

Volume

64

Issue

2

Start / End Page

225 / 232

Location

United States

Related Subject Headings

  • Receptors, Cytoplasmic and Nuclear
  • Quinine
  • Quinidine
  • Protein Binding
  • Mice
  • Macrophages, Peritoneal
  • Inositol 1,4,5-Trisphosphate Receptors
  • Inositol 1,4,5-Trisphosphate
  • Chloroquine
  • Cell Compartmentation
 

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Misra, U. K., Gawdi, G., & Pizzo, S. V. (1997). Chloroquine, quinine and quinidine inhibit calcium release from macrophage intracellular stores by blocking inositol 1,4,5-trisphosphate binding to its receptor. J Cell Biochem, 64(2), 225–232. https://doi.org/10.1002/(sici)1097-4644(199702)64:2<225::aid-jcb6>3.0.co;2-z
Misra, U. K., G. Gawdi, and S. V. Pizzo. “Chloroquine, quinine and quinidine inhibit calcium release from macrophage intracellular stores by blocking inositol 1,4,5-trisphosphate binding to its receptor.J Cell Biochem 64, no. 2 (February 1997): 225–32. https://doi.org/10.1002/(sici)1097-4644(199702)64:2<225::aid-jcb6>3.0.co;2-z.
Misra, U. K., et al. “Chloroquine, quinine and quinidine inhibit calcium release from macrophage intracellular stores by blocking inositol 1,4,5-trisphosphate binding to its receptor.J Cell Biochem, vol. 64, no. 2, Feb. 1997, pp. 225–32. Pubmed, doi:10.1002/(sici)1097-4644(199702)64:2<225::aid-jcb6>3.0.co;2-z.
Journal cover image

Published In

J Cell Biochem

DOI

ISSN

0730-2312

Publication Date

February 1997

Volume

64

Issue

2

Start / End Page

225 / 232

Location

United States

Related Subject Headings

  • Receptors, Cytoplasmic and Nuclear
  • Quinine
  • Quinidine
  • Protein Binding
  • Mice
  • Macrophages, Peritoneal
  • Inositol 1,4,5-Trisphosphate Receptors
  • Inositol 1,4,5-Trisphosphate
  • Chloroquine
  • Cell Compartmentation