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The novel P2X7 receptor antagonist PKT100 improves cardiac function and survival in pulmonary hypertension by direct targeting of the right ventricle

Authors :
Marie Besnier
Thomas Hansen
Gemma A. Figtree
Michael Tsang
Meghan Finemore
Keyvan Karimi Galougahi
James O'Brien-Brown
Elijah Genetzakis
Kristen J. Bubb
Michael Kassiou
Belinda A. Di Bartolo
Source :
American journal of physiology. Heart and circulatory physiology. 319(1)
Publication Year :
2020

Abstract

This study demonstrates the therapeutic potential for right-sided heart failure of a novel inhibitor of the P2X7 receptor (P2X7R). Inflammatory signaling and right ventricular function were improved in a mouse model of pulmonary fibrosis with secondary pulmonary hypertension when treated with this inhibitor. Importantly, survival was also improved, suggesting that this inhibitor, and other P2X7R antagonists, could be uniquely effective in right ventricle (RV)-targeted therapy in pulmonary hypertension. This addresses a major limitation of current treatment options, where the significant improvements in pulmonary pressures ultimately do not prevent mortality due to RV failure.

Details

ISSN :
15221539
Volume :
319
Issue :
1
Database :
OpenAIRE
Journal :
American journal of physiology. Heart and circulatory physiology
Accession number :
edsair.doi.dedup.....37b9b77deb2447954ab1ca4f288f961c