Sak K, Samuel K, Kelve M, Webb T E
Institute of Chemical Physics, Tartu University, 2 Jakobi St., 51014, Tartu, Estonia.
Eur J Pharmacol. 2001 Mar;415(2-3):127-33. doi: 10.1016/s0014-2999(01)00845-7.
In the present study, the P2Y receptor(s) mediating the effects of the pyrimidines UTP and UDP on phospholipase C activation in the mouse neuroblastoma x rat glioma hybrid cell line NG108-15 was investigated. Reverse Transcriptase-Polymerase Chain Reaction (RT-PCR) analysis detected transcripts for the P2Y(6) and P2Y(2) receptors, but not for P2Y(1) and P2Y(4.) UTP and UDP were equipotent agonists and their effects were partially additive. Suramin, reactive blue 2 and pyridoxal phosphate-6-azophenyl-2',4'disulfonic acid (PPADS) antagonised the phospholipase C response to both UTP and UDP. High micromolar concentrations of adenosine, 2-p-(2-carboxyethyl)phenethylamino-5'-N-ethylcarboxamidoadenosine (CGS-21680), 2',3'-O-isopropylideneadenosine (iPAdo) and adenosine 3':5'-cyclic monophosphate (3',5'-cAMP) were able to antagonise the effect of UTP on phospholipase C but not that of UDP. The additivity of the UTP and UDP responses, novel P2 receptor antagonist profile and the distinguishing action of adenosine may indicate the expression of a pyrimidine selective P2Y receptor in addition to the P2Y(6) type in these cells.
在本研究中，我们对介导嘧啶类物质尿苷三磷酸（UTP）和尿苷二磷酸（UDP）对小鼠神经母细胞瘤与大鼠胶质瘤杂交细胞系NG108-15中磷脂酶C激活作用的P2Y受体进行了研究。逆转录聚合酶链反应（RT-PCR）分析检测到了P2Y(6)和P2Y(2)受体的转录本，但未检测到P2Y(1)和P2Y(4)受体的转录本。UTP和UDP是等效激动剂，它们的作用部分具有相加性。苏拉明、活性蓝2和磷酸吡哆醛-6-偶氮苯基-2',4'-二磺酸（PPADS）拮抗了磷脂酶C对UTP和UDP的反应。高微摩尔浓度的腺苷、2-对-(2-羧乙基)苯乙氨基-5'-N-乙基羧酰胺腺苷（CGS-21680）、2',3'-O-异丙叉腺苷（iPAdo）和腺苷3':5'-环磷酸（3',5'-cAMP）能够拮抗UTP对磷脂酶C的作用，但不能拮抗UDP的作用。UTP和UDP反应的相加性、新型P2受体拮抗剂谱以及腺苷的区别作用可能表明，除了这些细胞中的P2Y(6)型受体外，还存在一种嘧啶选择性P2Y受体。
