Center for CardioVascular and Nutrition Research, INSERM, INRAE, Aix-Marseille University, 13005 Marseille, France.
Laboratory of Biochemistry, Assistance Publique des Hopitaux, 13005 Marseille, France.
Int J Mol Sci. 2021 Jul 15;22(14):7584. doi: 10.3390/ijms22147584.
While the concept of a receptor reserve (spare receptors) is old, their presence on human cells as an adaptive mechanism in cardiovascular disease is a new suggestion. The presence of spare receptors is suspected when the activation of a weak fraction of receptors leads to maximal biological effects, in other words, when the half-maximal effective concentration (EC) for a biological effect (cAMP production, for example) is lower than the affinity (K) of the ligand for a receptor. Adenosine is an ATP derivative that strongly impacts the cardiovascular system via its four membrane receptors, named AR, AR, AR, and AR, with the AR being more particularly involved in heart rhythm, while the AR controls vasodilation. After a general description of the tools necessary to explore the presence of spare receptors, this review focuses on the consequences of the presence of spare adenosine receptors in cardiovascular physiopathology. Finally, the role of the adenosinergic system in the long-term potentiation and its possible consequences on the physiopathology are also mentioned.
虽然受体储备(备用受体)的概念由来已久,但它们作为心血管疾病中的一种适应机制存在于人体细胞中,这是一个新的观点。当激活一小部分受体就能产生最大的生物学效应时,就怀疑存在备用受体,换句话说,当产生生物学效应(例如 cAMP 产生)的半效浓度(EC)低于配体与受体的亲和力(K)时,就怀疑存在备用受体。腺苷是一种 ATP 衍生物,通过其四个细胞膜受体(AR、AR、AR 和 AR)强烈影响心血管系统,其中 AR 更特别地参与心脏节律,而 AR 控制血管舒张。在对探索备用受体存在所需的工具进行了一般性描述之后,本篇综述重点介绍了备用腺苷受体在心血管病理生理学中的后果。最后,还提到了腺苷能系统在长期增强及其对病理生理学可能产生的影响的作用。