Haloperidol, a Sigma-1 Receptor Antagonist, Inhibits Ca2+ Responses in Rat Peritoneal Macrophages

Sigma-1 receptors are ubiquitous multifunctional ligand-regulated molecular chaperons in the membrane of the endoplasmic reticulum, having a unique history, structure and pharmacological profile. Sigma-1 receptors modulate a wide range of cellular processes in normal and pathological conditions, inc...

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Bibliographic Details
Published in:Biophysics (Oxford) 2023, Vol.68 (4), p.552-560
Main Authors: Milenina, L. S., Krutetskaya, Z. I., Antonov, V. G., Krutetskaya, N. I.
Format: Article
Language:English
Subjects:
Biological and Medical Physics
Biophysics
Ca2+-transporting ATPase
Calcium (intracellular)
Calcium antagonists
Calcium influx
Calcium signalling
Cell Biophysics
Cyclopiazonic acid
Endoplasmic reticulum
Haloperidol
Immunomodulation
Intracellular
Macrophages
Peritoneum
Physics
Physics and Astronomy
Thapsigargin
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Summary:Sigma-1 receptors are ubiquitous multifunctional ligand-regulated molecular chaperons in the membrane of the endoplasmic reticulum, having a unique history, structure and pharmacological profile. Sigma-1 receptors modulate a wide range of cellular processes in normal and pathological conditions, inclu-ding Ca 2+ signaling processes. Using the Fura-2AM fluorescent Ca 2+ probe, we have shown that sigma-1 receptor antagonist neuroleptic haloperidol significantly suppressed the mobilization of Ca 2+ from intracellular Ca 2+ stores and the subsequent store-dependent Ca 2+ entry into cells caused by endoplasmic Ca 2+ -ATPase inhibitors thapsigargin and cyclopiazonic acid, as well as immunomodulators glutoxim and molixan in rat peritoneal macrophages. The results indicated the participation of sigma-1 receptors in the complex signaling cascade caused by glutoxim or molixan and leading to an increase in intracellular Ca 2+ concentration in macrophages, as well as the involvement of sigma-1 receptors in the regulation of store-dependent Ca 2+ entry in macrophages.
ISSN:0006-3509
1555-6654
DOI:10.1134/S0006350923040140