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Real-time Live-cell Flow Cytometry to Investigate Calcium Influx, Pore Formation, and Phagocytosis by P2X7 Receptors in Adult Neural Progenitor Cells
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The P2X7 receptor channel: recent developments and the use of P2X7 antagonists in models of disease

Rachael Bartlett1, Leanne Stokes1, Ronald Sluyter2

  • 1School of Biological Sciences, University of Wollongong, New South Wales, Australia and Illawarra Health and Medical Research Institute, Wollongong, New South Wales, Australia (R.B., R.S.); and Health Innovations Research Institute, School of Medical Sciences, RMIT University, Bundoora, Victoria, Australia (L.S.).

Pharmacological Reviews
|June 15, 2014
PubMed

Insights

P2X7 receptor antagonists show promise for treating inflammatory, immune, and neurologic disorders. This review summarizes their use in preclinical models and ongoing human clinical trials, highlighting P2X7 as a therapeutic target.

Area of Science:

  • Immunology
  • Neuroscience
  • Pharmacology

Background:

  • The P2X7 receptor (P2X7) is an ATP-gated ion channel primarily on immune cells.
  • P2X7 activation influences inflammation, cell death, and proliferation, implicating it in various diseases.

Purpose of the Study:

  • This review focuses on P2X7 antagonists in preclinical models of neurologic, inflammatory, and musculoskeletal disorders.
  • It also covers P2X7 characterization, variants, signaling, and therapeutic potential.

Main Methods:

  • The review synthesizes data from rodent models of disease and injury.
  • It discusses P2X7 cloning, characterization across species, and genetic variations.
  • Emerging signaling pathways and modulators of P2X7 are also examined.

Main Results:

  • P2X7 antagonists have demonstrated efficacy in numerous rodent disease models.
  • The review details P2X7 gating, permeability, and polymorphic/splice variants.
  • Preclinical data supports P2X7's role in diverse pathological conditions.

Conclusions:

  • P2X7 antagonists are a promising therapeutic strategy for various diseases.
  • Further research into P2X7 signaling and modulators will advance its clinical application.
  • Clinical trials are underway, exploring P2X7's potential as a drug target.

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