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首页> 外文期刊>Japanese Journal of Pharmacology >Inhibitory Effect of EGTA on Serotonin Transport into Rabbit Blood Platelets: Possible Involvement of the Glycoprotein IIb/IIIa Complex
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Inhibitory Effect of EGTA on Serotonin Transport into Rabbit Blood Platelets: Possible Involvement of the Glycoprotein IIb/IIIa Complex

机译:EGTA对5-羟色胺转运入兔血小板的抑制作用:糖蛋白IIb / IIIa复合物的可能参与

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References(15) We reported previously that serotonin (5-HT) transport was attenuated by treatment of platelets with EGTA, and that this inhibitory effect of EGTA was restored by CaCl2• In the present study, the inhibitory effect of EGTA was found to be uncompetitive, and no inhibitory effect was observed when EGTA was added at 20°C. Genistein and thyrphostin A47, both protein tyrosine kinase inhibitors, inhibited Ca2+-induced restoration of 5-HT transport. In contrast, the protein tyrosine phosphatase inhibitor phenylarsine oxide significantly augmented Ca2+-induced restoration of 5-HT transport. These results might support the hypothesis that the glycoprotein (GP) Ilb/IIIa complex, a platelet membrane integrin protein, might regulate 5-HT transport into blood platelets. It is conceivable that Ca2+ chelation by EGTA might cause temperature-dependent dissociation of the GP IIb/IIIa complex, which results in the reduction of 5-HT transport. Rearrangement of the GP IIb/IIIa complex by replenishment of the Ca2+ binding sites might restore the EGTA-induced reduction of 5-HT transport.
机译:参考文献(15)我们先前曾报道过用EGTA处理血小板会减弱5-羟色胺(5-HT)的转运,而CaCl2恢复了EGTA的这种抑制作用。在本研究中,发现EGTA的抑制作用是无竞争性,在20°C加入EGTA时未观察到抑制作用。染料木素和甲状腺素A47都是蛋白酪氨酸激酶抑制剂,它们抑制Ca2 +诱导的5-HT转运恢复。相反,蛋白质酪氨酸磷酸酶抑制剂苯inhibitor氧化物大大增强了Ca2 +诱导的5-HT转运的恢复。这些结果可能支持以下假设:糖蛋白(GP)Ilb / IIIa复合物(一种血小板膜整联蛋白)可能会调节5-HT向血小板的转运。可以想象,EGTA的Ca2 +螯合可能导致GP IIb / IIIa复合物的温度依赖性解离,从而导致5-HT转运减少。通过补充Ca2 +结合位点对GP IIb / IIIa复合物进行重排可能会恢复EGTA诱导的5-HT转运减少。

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