Ayme-Dietrich Estelle, Aubertin-Kirch Gaëlle, Maroteaux Luc, Monassier Laurent
Laboratoire de neurobiologie et pharmacologie cardiovasculaire (EA7296), faculté de médecine, fédération de médecine translationnelle, laboratoire de neurobiologie et pharmacologie cardiovasculaire (EA7296), université et centre hospitalier de Strasbourg, 67085 Strasbourg, France.
Inserm UMR-S 839, institut du Fer-à-Moulin, Sorbonne université, UPMC université Paris 06, 75005 Paris, France.
Arch Cardiovasc Dis. 2017 Jan;110(1):51-59. doi: 10.1016/j.acvd.2016.08.002. Epub 2016 Dec 21.
Plasma 5-hydroxytryptamine (5-HT; serotonin), released from blood platelets, plays a major role in the human cardiovascular system. Besides the effect of endogenous serotonin, many drugs targeting serotonergic receptors are widely used in the general population (antiobesity agents, antidepressants, antipsychotics, antimigraine agents), and may enhance the cardiovascular risk. Depending on the type of serotonin receptor activated and its location, the use of these compounds triggers acute and chronic effects. The acute cardiovascular response to 5-HT, named the Bezold-Jarish reflex, leads to intense bradycardia associated with atrioventricular block, and involves 5-HT, 5-HT, 5-HT and 5-HT receptors. The chronic contribution of 5-HT and its receptors (5-HT and 5-HT) in cardiovascular tissue remodeling, with a particular emphasis on cardiac hypertrophy, fibrosis and valve degeneration, will be explored in this review. Finally, through the analysis of the effects of sarpogrelate, some new aspects of 5-HT receptor pharmacology in vasomotor tone regulation and the interaction between endothelial and smooth muscle cells will also be discussed. The aim of this review is to emphasize the cardiac side effects caused by serotonin receptor activation, and to highlight their possible prevention by the development of new drugs targeting this system.
从血小板释放的血浆5-羟色胺（5-HT；血清素）在人体心血管系统中起主要作用。除了内源性血清素的作用外，许多靶向血清素能受体的药物在普通人群中广泛使用（抗肥胖药、抗抑郁药、抗精神病药、抗偏头痛药），可能会增加心血管风险。根据激活的血清素受体类型及其位置，这些化合物的使用会引发急性和慢性效应。对5-HT的急性心血管反应，即贝佐尔德-雅里什反射，会导致与房室传导阻滞相关的强烈心动过缓，涉及5-HT、5-HT、5-HT和5-HT受体。本综述将探讨5-HT及其受体（5-HT和5-HT）在心血管组织重塑中的慢性作用，尤其侧重于心脏肥大、纤维化和瓣膜退变。最后，通过分析沙格雷酯的作用，还将讨论5-HT受体药理学在血管舒缩张力调节以及内皮细胞和平滑肌细胞之间相互作用方面的一些新情况。本综述的目的是强调血清素受体激活引起的心脏副作用，并突出通过开发靶向该系统的新药来预防这些副作用的可能性。
