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The σ1 receptor is a target for the development of cardioprotective drugs

Leonid N Maslov1, Kirill Tsirulnikov2, Alisa S Slidnevskaya3

  • 1Cardiology Research Institute, National Research Medical Center, Russian Academy of Sciences, Tomsk, Russia.

Life Sciences
|October 9, 2025
PubMed

Insights

Sigma-1 receptor agonists show promise for treating acute myocardial infarction (AMI) and cardiogenic shock. These compounds protect the heart from reperfusion injury and prevent adverse cardiac remodeling.

Area of Science:

  • Cardiovascular Research
  • Pharmacology
  • Cell Biology

Background:

  • Acute myocardial infarction (AMI) has a significant in-hospital mortality rate (4.6%-7.5%).
  • Reperfusion cardiac injury (RCI) and cardiogenic shock are major causes of death in AMI patients.
  • Investigating sigma-1 (σ1) receptor agonists offers potential therapeutic strategies for RCI.

Purpose of the Study:

  • To explore the cardiovascular effects of sigma-1 (σ1) receptor agonists.
  • To assess the potential of σ1 receptor agonists in treating AMI, cardiogenic shock, and preventing cardiac remodeling.

Main Methods:

  • Literature search conducted using the PubMed database.
  • Review of studies on sigma-1 receptor expression and function in cardiac cells.
  • Analysis of the effects of σ1 receptor agonists on cardiomyocyte contractility, cardiac remodeling, and apoptosis.

Main Results:

  • Sigma-1 receptors are present in cardiomyocytes and endothelial cells, located in the cell membrane, ER, and mitochondria.
  • σ1 receptor agonists enhance cardiomyocyte contractility and mitigate adverse cardiac remodeling.
  • Activation of σ1 receptors inhibits cardiomyocyte apoptosis during ischemia/reperfusion and promotes cardioprotective pathways.

Conclusions:

  • Sigma-1 receptor agonists demonstrate potential as a basis for novel therapeutics for AMI and cardiogenic shock.
  • These agonists may also be valuable in preventing adverse cardiac remodeling post-AMI.
  • Further research into σ1 receptor agonists could lead to improved treatments for cardiovascular diseases.
Abstract

Keywords:
Cardiac remodelingHeartIschemia/reperfusionMitochondriaσ(1)-Receptor

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