Perspective Cardiac P2X4 Receptors Targets in Ischemia and Heart Failure?

Targets in Ischemia and Heart Failure?

Purinergic1 receptors were initially conceived to describe the likely existence of membrane receptors responding to adenosine triphosphate (ATP) (P2 receptors) or its breakdown product adenosine (P1 receptors) in causing nonadrenergic, noncholinergic relaxation of gut smooth muscle.1 Cloning of these receptors has yielded insights into their properties and signaling mechanisms, allowing classif...

A Novel Protective Role of Endogenous Cardiac Myocyte P2X4 Receptors in Heart Failure Yang et al: Myocyte P2X4 Receptors in Heart Failure

A beneficial role of cardiac P2X4 receptors in heart failure: rescue of the calsequestrin overexpression model of cardiomyopathy.

The P2X4 purinergic receptor (P2X4R) is a ligand-gated ion channel. Its activation by extracellular ATP results in Ca2+ influx. Transgenic cardiac overexpression of the human P2X4 receptor showed an in vitro phenotype of enhanced basal contractility. The objective here was to determine the in vivo cardiac physiological role of this receptor. Specifically, we tested the hypothesis that this rece...

Role of P2X purinergic receptors in the rescue of ischemic heart failure.

Evidence is accumulating to support the presence of P2X purinergic receptors in the heart. However, the biological role of this receptor remains to be defined. The objectives here were to determine the role of cardiac P2X receptors in modulating the progression of post-myocardial infarction ischemic heart failure and to investigate the underlying mechanism. The P2X4 receptor (P2X4R) is an impor...

Novel protective role of endogenous cardiac myocyte P2X4 receptors in heart failure.

BACKGROUND Heart failure (HF), despite continuing progress, remains a leading cause of mortality and morbidity. P2X4 receptors (P2X4R) have emerged as potentially important molecules in regulating cardiac function and as potential targets for HF therapy. Transgenic P2X4R overexpression can protect against HF, but this does not explain the role of native cardiac P2X4R. Our goal is to define the ...