Vascular Functional Effects of the Apelinergic System


İŞBİL N., ŞAHİNTÜRK S., DEMİREL S.

Literatür Eczacılık Bilimleri Dergisi, vol.10, no.1, pp.12-20, 2021 (Peer-Reviewed Journal) identifier

Abstract

The apelinergic system consists of apelin, elabela, andtheir common receptor apelin receptor (APJ). APJ is a G protein-coupled receptor. Apelin is the first discovered endogenous APJ ligand.Later, elabela was discovered and added to the system. Apelinergicsystem components have a widespread expression in the human body.The apelinergic system which plays a role in many physiological processes such as body-fluid homeostasis, energy metabolism, and regulation of cardiac contractility participates in the regulation ofvascular tone and blood pressure. Apelin and elabela, which have similar effects on vascular tone, differ in their effect mechanisms. APJ isexpressed in both vascular endothelial cells and vascular smooth muscle cells. This situation is important because it mediates the oppositeeffects in vascular tension. Apelin usually has a vasodilator effectthrough the activation of the endothelial nitric oxide synthase/nitricoxide (NO) pathway in physiological conditions. However, in the absence of a functional endothelium, apelin causes vasoconstriction.Elabela has a vasodilator effect similar to apelin, but it is thought thatNO has no role in the vasodilator effect of elabela. When apelin andelabela are administered peripherally, they usually lower blood pressure and exhibit an antihypertensive effect. Therefore, the apelinergicsystem has great potential to develop alternative agents for the treatment of hypertensive diseases such as essential hypertension and pulmonary hypertension. The half-lives of apelin and elabela are quiteshort, and current studies have focused on developing longer-actingapelinergic analogs. In this review, we focused on the vascular functional effects and effect mechanisms of the apelinergic system