P2X7 receptor in cardiovascular disease: The heart side
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Updated: Jan 28, 2026

Dissection Techniques and Histological Sampling of the Heart in Large Animal Models for Cardiovascular Diseases
Published on: June 16, 2022
1Department of Microbial Pathogenesis and Immunology, Texas A&M University, College Station, Texas.
Abstract:
The P2X7 receptor is a ligand-gated purinergic receptor activated by extracellular ATP. The receptor is highly expressed in immune cells and in the brain, and, upon activation, the P2X7 receptor allows a cation flux, leading to the distinct activation of intracellular signalling pathways as the secretion of pro-inflammatory cytokines, and modulation of cell survival. Through these molecular mechanisms, P2X7 is known to play important roles in physiology and pathophysiology of a wide spectrum of diseases, including cancer, inflammatory diseases, neurological, respiratory and more recently cardiovascular diseases. Recent studies demonstrated that the P2X7 could modulate the assembly of the NLRP3 inflammasome, leading to the secretion of pro-inflammatory factors and worsen the cardiac disease phenotypes. This review discusses the critical molecular function of P2X7 in the modulation of the onset, progression and resolution of cardiovascular diseases and analyses the putative future use of P2X7-based therapies that modulate the IL-1β secretion arm and direct P2X7 antagonists.
Insights
The P2X7 receptor, crucial in immune cells and the brain, influences cardiovascular diseases. Targeting P2X7 offers potential therapies for conditions like heart disease by modulating inflammation.
Area of Science:
- Immunology
- Cardiovascular Biology
- Molecular Medicine
Background:
- The P2X7 receptor (P2X7R) is a ligand-gated ion channel activated by extracellular ATP.
- It is expressed in immune cells and the brain, regulating intracellular signaling, cytokine secretion, and cell survival.
- P2X7R plays roles in various diseases, including cardiovascular conditions.
Purpose of the Study:
- To review the molecular function of P2X7R in cardiovascular diseases.
- To analyze the role of P2X7R in NLRP3 inflammasome activation and associated inflammation.
- To explore P2X7R-based therapeutic strategies for cardiovascular diseases.
Main Methods:
- Literature review of studies on P2X7R in cardiovascular pathophysiology.
- Analysis of P2X7R's role in inflammasome assembly and cytokine secretion.
- Evaluation of P2X7R antagonists and IL-1β modulation as therapeutic approaches.
Main Results:
- P2X7R activation leads to cation flux, influencing pro-inflammatory cytokine secretion.
- P2X7R modulates NLRP3 inflammasome assembly, exacerbating cardiac disease phenotypes.
- Recent studies highlight P2X7R's involvement in the onset, progression, and resolution of cardiovascular diseases.
Conclusions:
- P2X7R is a key regulator in cardiovascular disease pathogenesis.
- Modulating P2X7R, particularly its IL-1β secretion pathway, presents a promising therapeutic avenue.
- P2X7R antagonists offer potential for treating inflammatory cardiovascular conditions.
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