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苏拉明和活性蓝2是大鼠巨核细胞上新发现的嘌呤受体的拮抗剂。

Suramin and reactive blue 2 are antagonists for a newly identified purinoceptor on rat megakaryocyte.

作者信息

Uneyama H, Uneyama C, Ebihara S, Akaike N

机构信息

Department of Neurophysiology, Tohoku University School of Medicine, Sendai, Japan.

出版信息

Br J Pharmacol. 1994 Jan;111(1):245-9. doi: 10.1111/j.1476-5381.1994.tb14051.x.

Abstract
  1. The effects of purinoceptor antagonists on ATP-induced oscillatory K(+)-currents in rat isolated megakaryocytes were investigated. 2. Both reactive blue-2 (RB-2), a selective antagonist of the P2Y purinoceptor, purinoceptor, at concentrations of 0.3-10 microM and suramin, a non-selective P2 purinoceptor antagonist, at 1-30 microM blocked the ATP-induced oscillation in a concentration-dependent manner. 3. RB-2 and suramin also blocked the ADP-induced K(+)-current oscillation at the same concentration range as in the case of ATP. However, both suramin and RB-2 had no effect on thrombin- and inositol 1,4,5-trisphosphate (IP3)-induced K+ current oscillation, indicating that they act as specific purinoceptor antagonists. 4. Thus, the purinoceptors on megakaryocytes show the properties of the P2 subtype according to their blockade by antagonists.
摘要
  1. 研究了嘌呤受体拮抗剂对大鼠分离巨核细胞中ATP诱导的振荡性钾电流的影响。2. 选择性P2Y嘌呤受体拮抗剂活性蓝-2(RB-2)在浓度为0.3 - 10微摩尔时,以及非选择性P2嘌呤受体拮抗剂苏拉明在1 - 30微摩尔时,均以浓度依赖性方式阻断ATP诱导的振荡。3. RB-2和苏拉明在与ATP相同的浓度范围内也阻断ADP诱导的钾电流振荡。然而,苏拉明和RB-2对凝血酶和肌醇1,4,5 - 三磷酸(IP3)诱导的钾电流振荡均无影响,表明它们作为特异性嘌呤受体拮抗剂起作用。4. 因此,根据拮抗剂对巨核细胞上嘌呤受体的阻断作用,这些嘌呤受体表现出P2亚型的特性。

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