Different sedimentation properties of agonist- and antagonist-labelled platelet alpha 2 adrenergic receptors.
Different sedimentation properties of agonist- and antagonist-labelled platelet alpha 2 adrenergic receptors.
复制标题
激动剂和拮抗剂标记的血小板 α2 肾上腺素受体的不同沉降特性。
DOI：
10.1016/0006-291x(81)91941-0
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发表时间：
1981
影响因子：
3.1
通讯作者：
Caron,MG
中科院分区：
文献类型：
--
作者：
Michel,T;Hoffman,BB;Lefkowitz,RJ;Caron,MG
用地黄苷溶解人血小板颗粒制剂中的α 2肾上腺素能受体。溶解后的alpha2受体保留了膜结合受体的基本结合特异性特征。alpha2受体可以用激动剂（[3H]肾上腺素）或拮抗剂（[3H]育亨宾）放射性配体在血小板膜上标记。当这些膜被洋地黄苷溶解并在蔗糖密度梯度上离心时，激动剂标记受体的沉降系数（14.6S）大于拮抗剂标记受体的沉降系数（12.9S）。这一观察结果可能为α 2肾上腺素能受体抑制腺苷酸环化酶的机制提供了新的思路。
Alpha2adrenergic receptors were solubilized from human platelet particulate preparations with digitonin. The solubilized alpha2receptors retained the essential binding specificity characteristics of the membrane-bound receptors. The alpha2receptors could be labelled in platelet membranes with either agonist ([3H]epinephrine) or antagonist ([3H]yohimbine) radioligands. When these membranes were solubilized with digitonin and centrifuged on sucrose density gradients, the sedimentation coefficient of the agonist-labelled receptor (14.6S) was greater than that of the antagonist-labelled receptor (12.9S). This observation may provide insight into the mechanism of adenylate cyclase inhibition by alpha2adrenergic receptors.