A P2X7 receptor antagonist attenuates experimental autoimmune myocarditis via suppressed myocardial CD4+ T and macrophage infiltration and NADPH oxidase 2/4 expression in mice

Heart Vessels. 2015 Jul;30(4):527-33. doi: 10.1007/s00380-014-0527-2. Epub 2014 May 31.

Abstract

Myocarditis is a clinically serious disease; however, no effective treatment has been elucidated. The P2X7 receptor is related to the pathophysiology of inflammation in many cardiovascular diseases. The P2X7 receptor antagonist is promising as an immunosuppressive treatment; however, its role in myocarditis is still to be established. To clarify the role of the P2X7 receptor, we used a murine experimental autoimmune myocarditis (EAM) model. Mice were immunized on day 0 and 7 with synthetic cardiac myosin peptide to establish EAM. The mice with induced EAM were treated with A740003, the P2X7 receptor antagonist (n = 10), or not treated (n = 11); hearts were harvested on day 21. The P2X7 receptor antagonist improved myocardial contraction of the EAM hearts via suppressed infiltration of CD4+ T cells and macrophages. Similarly, mRNA expression of interleukin 1 beta, the P2X7 receptor and NADPH oxidase 2/4 was lower in the heart of the P2X7 receptor antagonist-treated group compared to the non-treat group. The P2X7 receptor antagonist suppressed EAM development; thus, this inhibition is promising for treating clinical myocarditis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetamides / therapeutic use*
  • Animals
  • Autoimmune Diseases / drug therapy*
  • Disease Models, Animal
  • Inflammation / metabolism
  • Macrophages / metabolism
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Myocarditis / drug therapy*
  • Myocardium / pathology
  • NADPH Oxidases / metabolism*
  • Purinergic P2X Receptor Antagonists / therapeutic use*
  • Quinolines / therapeutic use*
  • Receptors, Purinergic P2X7 / metabolism

Substances

  • (N-(1-(((cyanoimino)(5-quinolinylamino) methyl) amino)-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide)
  • Acetamides
  • Purinergic P2X Receptor Antagonists
  • Quinolines
  • Receptors, Purinergic P2X7
  • NADPH Oxidases