Apelin is a vasoactive peptide and is an endogenous ligand for APJ receptors, which are widely expressed in blood vessels, heart, and cardiovascular regulatory regions of the brain. A growing body of evidence now demonstrates a regulatory role for the apelin/APJ receptor system in cardiovascular physiology and pathophysiology, thus making it a potential target for cardiovascular drug discovery and development. Indeed, ongoing studies are investigating the potential benefits of apelin and apelin-mimetics for disorders such as heart failure and pulmonary arterial hypertension. Apelin causes relaxation of isolated arteries, and systemic administration of apelin typically results in a reduction in systolic and diastolic blood pressure and an increase in blood flow. Nonetheless, vasopressor responses and contraction of vascular smooth muscle in response to apelin have also been observed under certain conditions. The goal of the current review is to summarize major findings regarding the apelin/APJ receptor system in blood vessels, with an emphasis on regulation of vascular tone, and to identify areas of investigation that may provide guidance for the development of novel therapeutic agents that target this system.

Apelin是一种血管活性肽，是APJ受体的内源性配体，APJ受体在脑的血管，心脏和心血管调节区域广泛表达。现在越来越多的证据表明，apelin / APJ受体系统在心血管生理和病理生理中具有调节作用，因此使其成为心血管药物发现和开发的潜在靶标。实际上，正在进行的研究正在研究apelin和apelin模拟物对诸如心力衰竭和肺动脉高压等疾病的潜在益处。Apelin引起孤立的动脉舒张，而apelin的全身给药通常会导致收缩压和舒张压降低，血流增加。尽管如此，在某些情况下，还观察到了血管加压药反应和对apelin的反应，血管平滑肌的收缩。本综述的目的是总结有关血管中apelin / APJ受体系统的主要发现，重点是调节血管紧张度，并确定可为开发靶向新治疗剂提供指导的研究领域这个系统。