Assessment of binding indices and physiological responsiveness of the 5-HT2 receptor on human platelets.
Assessment of binding indices and physiological responsiveness of the 5-HT2 receptor on human platelets.
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评估 5-HT2 受体对人血小板的结合指数和生理反应性。
DOI：
10.1016/0024-3205(87)90091-9
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发表时间：
1987
期刊：
影响因子：
6.1
通讯作者：
Sweeney,JA
中科院分区：
文献类型：
--
作者：
McBride,PA;Mann,JJ;Polley,MJ;Wiley,AJ;Sweeney,JA
这是第一个报告的平行研究的结合指数和生理反应的“5-羟色胺2”（5-HT 2）受体对人血小板膜。结合指数通过微量测定法测量，采用[125 I] ILSD作为放射性配体和酮色林以确定特异性结合。在健康人中发现了一个单一受体群体，其特征在于KD为1.69 ± 0.45 nM，Bmax为14.5 ± 6.0 pmol/g蛋白。用阈浓度二磷酸腺苷（ADP）诱导的测定来评价血小板5-HT 2受体复合物的功能反应性。血小板5-HT_2受体位点数（Bmax）与血小板聚集反应强度呈显著正相关（r = 70，n = 38，p<0.001）。评估5-HT 2受体复合物应有助于研究血小板5-HT 2受体复合物应有助于研究年龄、激素、疾病和药物对人类受试者5-HT 2受体功能的影响。
This is the first report of parallel studies of binding indices and physiological responsiveness of the “Serotonin-two” (5-HT2) receptor on the human platelet membrane. Binding indices were measured by a microassay employing [125I] ILSD as radioligand and ketanserin to define specific binding. A single receptor population was found, characterized by a KDof 1.69 ± 0.45 nM and Bmaxof14.5 ± 6.0 pmol/g protein in healty subjects. Functioning responsiveness of the platelet 5-HT2receptor complex was assessed by measurement induced by threshold concentrations of adenosine diphosphate (ADP). A statistically significant positive correlation was found between the number of platelet 5-HT2receptor sites (Bmax) and the magnitude of the serotonin-amplified aggregation response (r = 70, n = 38, p<0.001). Assessment 5-HT2receptor complex should facilitate study of of the platelet 5-HT2receptor complex should facilitate study of age, hormonal, disease, and drug effects on 5-HT2receptor function in human subjects.