Charlton S J, Brown C A, Weisman G A, Turner J T, Erb L, Boarder M R
Department of Cell Physiology and Pharmacology, University of Leicester.
Br J Pharmacol. 1996 Dec;119(7):1301-3. doi: 10.1111/j.1476-5381.1996.tb16038.x.
The P2Y family of receptors are G protein-coupled receptors for ATP, ADP, UTP and UDP. Recently several members of this family have been cloned, including the P2Y4, which is activated by UTP but not by ATP. In the present report, using receptors stably transfected into 1321N1 cells, we show that suramin acts as an antagonist at cloned P2Y1 and (less potently) P2Y2 receptors, but not at the cloned P2Y4 receptor. Furthermore, PPADS (pyridoxal-phosphate-6-azophenyl-2',4'-disulphonic acid), a potent antagonist at the P2Y1 receptor, is a relatively inneffective antagonist at the cloned P2Y4 receptor. This work moves us closer to the goal of classifying the native P2Y receptors on the basis of agonist and antagonist profiles.
P2Y 受体家族是针对三磷酸腺苷（ATP）、二磷酸腺苷（ADP）、三磷酸尿苷（UTP）和二磷酸尿苷（UDP）的 G 蛋白偶联受体。最近，该家族的几个成员已被克隆，包括 P2Y4，它可被 UTP 激活，但不能被 ATP 激活。在本报告中，我们使用稳定转染到 1321N1 细胞中的受体，发现苏拉明在克隆的 P2Y1 受体和（效力较弱的）P2Y2 受体上起拮抗剂作用，但在克隆的 P2Y4 受体上不起作用。此外，P2Y1 受体的强效拮抗剂吡哆醛 - 磷酸 -6- 偶氮苯 -2',4'- 二磺酸（PPADS）在克隆的 P2Y4 受体上是相对无效的拮抗剂。这项工作使我们更接近根据激动剂和拮抗剂谱对天然 P2Y 受体进行分类的目标。
