Van Der Giet Markus, Giebing Gunter, Tolle Markus, Schmidt Sven
Drug News Perspect. 2002 Dec;15(10):640-646. doi: 10.1358/dnp.2002.15.10.740237.
Extracellular nucleotides have been implicated in a number of physiological functions. Nucleotides act on cell-surface receptors known as P2 receptors, of which several subtypes have been cloned. P2X receptors are ligand-gated ion channels, whereas P2Y receptors belong to the superfamily of G-protein-coupled receptors. The human P2Y-receptor family is composed of seven subtypes (P2Y(1), P2Y(2), P2Y(4), P2Y(6), P2Y(11), P2Y(12), P2Y(13)). The principal physiological agonists of the human P2Y receptors are ADP (P2Y(1), P2Y(12), P2Y(13)), UTP/ATP (P2Y(2)), UTP (P2Y(4)), UDP (P2Y(6)) and ATP (P2Y(11)). P2Y receptors are widely expressed in human tissues, and many subtypes are found in vascular smooth muscle cells and endothelial cells in blood vessels. The intracellular signaling of P2Y receptors is very complex. Activation of P2Y receptors in blood vessels induces vasodilation or vasoconstriction, prolifera- tion of vascular smooth muscle cells and Ca(2+)-sensitization. All mechanisms play an important role in blood pressure control and cardiovascular disease. (c) 2002 Prous Science. All rights reserved.
细胞外核苷酸参与了多种生理功能。核苷酸作用于被称为P2受体的细胞表面受体,其中几种亚型已被克隆。P2X受体是配体门控离子通道,而P2Y受体属于G蛋白偶联受体超家族。人类P2Y受体家族由七种亚型组成(P2Y(1)、P2Y(2)、P2Y(4)、P2Y(6)、P2Y(11)、P2Y(12)、P2Y(13))。人类P2Y受体的主要生理激动剂是ADP(P2Y(1)、P2Y(12)、P2Y(13))、UTP/ATP(P2Y(2))、UTP(P2Y(4))、UDP(P2Y(6))和ATP(P2Y(11))。P2Y受体在人体组织中广泛表达,在血管的血管平滑肌细胞和内皮细胞中发现了许多亚型。P2Y受体的细胞内信号传导非常复杂。血管中P2Y受体的激活会诱导血管舒张或收缩、血管平滑肌细胞增殖和Ca(2+)敏化。所有这些机制在血压控制和心血管疾病中都起着重要作用。(c) 2002 Prous Science。保留所有权利。