Sigma-1 Receptor Ligands Chlorpromazine and Trifluoperazine Attenuate Ca2+ Responses in Rat Peritoneal Macrophages

Sigma-1 receptors are ubiquitous multifunctional ligand-regulated molecular chaperones in the endoplasmic reticulum membrane with a unique history, structure, and pharmacological profile. Sigma-1 receptors bind ligands of different chemical structure and pharmacological action and modulate a wide ra...

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Bibliographic Details
Published in:Cell and tissue biology 2022, Vol.16 (3), p.233-244
Main Authors: Milenina, L. S., Krutetskaya, Z. I., Antonov, V. G., Krutetskaya, N. I.
Format: Article
Language:English
Subjects:
Antipsychotics
Biomedical and Life Sciences
Calcium (intracellular)
Calcium signalling
Cell Biology
Chlorpromazine
Cyclopiazonic acid
Endoplasmic reticulum
Immunomodulation
Life Sciences
Ligands
Macrophages
Peritoneum
Phenothiazine
Thapsigargin
Trifluoperazine
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Summary:Sigma-1 receptors are ubiquitous multifunctional ligand-regulated molecular chaperones in the endoplasmic reticulum membrane with a unique history, structure, and pharmacological profile. Sigma-1 receptors bind ligands of different chemical structure and pharmacological action and modulate a wide range of cellular processes in health and disease, including Ca 2+ signaling. To elucidate the involvement of sigma-1 receptors in the processes of Ca 2+ signaling in macrophages we studied the effect of sigma-1 receptor ligands, phenothiazine neuroleptics chlorpromazine and trifluoperazine, on Ca 2+ responses induced by inhibitors of endoplasmic Ca 2+ –ATPases thapsigargin and cyclopiazonic acid, as well as by disulfide-containing immunomodulators Glutoxim and Molixan in rat peritoneal macrophages. Using Fura-2AM microfluorimetry we showed for the first time that chlorpromazine and trifluoperazine inhibit both phases of Ca 2+ responses induced by Glutoxim, Molixan, thapsigargin, and cyclopiazonic acid in rat peritoneal macrophages. The data obtained indicate the participation of sigma-1 receptors in a complex signaling cascade caused by Glutoxim or Molixan and leading to an increase in intracellular Ca 2+ concentration in macrophages. The results also indicate the involvement of sigma-1 receptors in the regulation of store-dependent Ca 2+ entry in macrophages.
ISSN:1990-519X
1990-5203
DOI:10.1134/S1990519X22030075