PPADS和苏拉明拮抗剂在克隆P2Y P2U-purinoceptors。

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查尔顿SJ,布朗CA,维斯曼GA,特纳JT, Erb L,寄宿生

PPADS和苏拉明拮抗剂在克隆P2Y P2U-purinoceptors。

Br J杂志。1996年6月,118 (3):704 - 10。

PubMed ID

8762097 (在PubMed

]

文摘

1。苏拉明的影响以及pyridoxalphosphate-6-azophenyl-2 ', 4 ' -disulphonic酸(PPADS) 1321年在刺激磷脂酶C n1与人类细胞转染P2U-purinoceptor (h - p2u - 1321 n1细胞)或土耳其P2Y-purinoceptor (t - p2y - 1321 n1细胞)进行了研究。2-Methylthioadenosine三磷酸(2 mesatp)被用来在t - p2y受体激动剂- 1321 n1细胞和尿苷三磷酸(UTP) h - p2u - 1321 n1细胞。2。苏拉明造成一个平行的转向右边的量效曲线在t - 2 mesatp p2y - 1321 n1细胞,产生席尔德阴谋斜率为1.16 + / - 0.08和回目值为5.77 + / - 0.11。3所示。苏拉明也转向正确的量效曲线引起的UTP的h - p2u - 1321 n1细胞,和席尔德情节给了边坡不同于团结(1.57 + / - 0.19)和一个明显的回目4.32 + / - 0.13的价值。苏拉明因此少比P2Y-purinoceptor P2U-purinoceptor强有力的对手。4所示。在ectonucleotidase抑制剂的存在,陆军研究实验室的67156 (6 n、N-diethyl-beta gamma-dibromomethylene-D-ATP)没有显著差异的EC50或形状曲线与细胞类型,和苏拉明回目值没有区别。 5. PPADS caused an increase in the EC50 for 2MeSATP in the t-P2Y-1321N1 cells. The Schild plot had a slope different from unity (0.55 +/- 0.15) and an X-intercept corresponding to an apparent pA2 of 5.98 +/- 0.65. 6. PPADS up to 30 microM had no effect on the concentration-response curve for UTP with the h-P2U-1321N1 cells. 7. In conclusion, suramin and PPADS show clear differences in their action at the 2 receptor types, in each case being substantially more effective as an antagonist at the P2Y-purinoceptor than at the P2U-purinoceptor. Ectonucleotidase breakdown had little influence on the nature of the responses at the two receptor types, or in their differential sensitivity to suramin.

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药物靶点

药物	目标	类	生物	药理作用	行动
苏拉明	P2Y purinoceptor 2	蛋白质	人类	是的	拮抗剂	细节