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首页> 外文期刊>Life sciences >The specific binding of the platelet-activating factor (PAF) receptor antagonist WEB 2086 and the benzodiazepine flunitrazepam to rat hepatocytes.
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The specific binding of the platelet-activating factor (PAF) receptor antagonist WEB 2086 and the benzodiazepine flunitrazepam to rat hepatocytes.

机译：血小板活化因子（PAF）受体拮抗剂WEB 2086和苯二氮卓类氟尼西epa与大鼠肝细胞的特异性结合。

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Thieno-triazolodiazepines WEB 2086 and BN 50739 have been described as the potent PAF receptor antagonists. Binding of radiolabeled [3H]WEB 2086 has been widely employed to characterize PAF receptors in different cells. In a search for a PAF receptor in isolated rat hepatocytes, we discovered that the binding of [3H]WEB to rat hepatocytes was highly specific but had a relatively low affinity with a Kd of 113 nM and Bmax of 0.65 pmol/10(6) cells in freshly isolated cell suspension and Kd of 1.65 muM and Bmax of 2.0 pmol/plate in cultured hepatocytes. No consistent specific binding of [3H]PAF itself was found in the same cell preparations. The binding of [3H]flunitrazepam in the presence of the peripheral type of benzodiazepine receptor antagonist Ro 5-4864 was saturated and exhibited a K(i) of 3.8 nM and Bmax of 3.5 pmol/plate. The central type of benzodiazepine receptor antagonist clonazepam was competed for the [3H]flunitrazepam binding, however with a much lower affinity. Various antagonists inhibited the binding of [3H]WEB 2086 with a rank order BN 50739Ro 5-4864 > or = clonazepam. Interestingly, bicuculline, specific antagonist of GABA(A) recognition sites, also significantly reduced the binding of [3H]WEB 2086. The binding of [3H]flunitrazepam was inhibited with a rank potency BN 50739WEB 2086. Taken together, these findings suggest that the specific binding of PAF receptor antagonists WEB 2086 and BN 50739 in rat hepatocytes does not involve PAF receptors and occurs via peripheral benzodiazepine and, possibly GABA(A) receptor sites.
机译：硫代三唑并二氮杂卓WEB 2086和BN 50739被描述为有效的PAF受体拮抗剂。放射性标记的[3H] WEB 2086的结合已广泛用于表征不同细胞中的PAF受体。在分离的大鼠肝细胞中寻找PAF受体时，我们发现[3H] WEB与大鼠肝细胞的结合具有高度特异性，但亲和力相对较低，Kd为113 nM，Bmax为0.65 pmol / 10（6）。新鲜分离的细胞悬液中的细胞，培养的肝细胞中的Kd为1.65μM，Bmax为2.0 pmol /板。在相同的细胞制剂中未发现[3H] PAF本身的一致特异性结合。在存在外围类型的苯二氮卓受体拮抗剂Ro 5-4864的情况下，[3H]氟硝西binding的结合达到饱和，K（i）为3.8 nM，Bmax为3.5 pmol /板。苯并二氮杂receptor受体拮抗剂氯硝西am的中心类型竞争[3H]氟硝西epa的结合，但是亲和力低得多。各种拮抗剂以等级顺序BN 50739 Ro 5-4864>或=氯硝西inhibit抑制[3H] WEB 2086的结合。有趣的是，双瓜氨酸是GABA（A）识别位点的特异性拮抗剂，也显着降低了[3H] WEB 2086的结合。[3H]氟尼西epa的结合受到了BN 50739 WEB 2086的强效抑制。研究结果表明，PAF受体拮抗剂WEB 2086和BN 50739在大鼠肝细胞中的特异性结合不涉及PAF受体，而是通过周围的苯二氮卓和可能的GABA（A）受体位点发生。

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