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使用[3H]酮色林证明猫血小板上的S2受体结合位点。

Demonstration of S2-receptor binding sites on cat blood platelets using [3H]ketanserin.

作者信息

Leysen J E, Gommeren W, De Clerck F

出版信息

Eur J Pharmacol. 1983 Mar 18;88(1):125-30. doi: 10.1016/0014-2999(83)90401-6.

Abstract

[3H]Ketanserin showed substantial binding to cat platelet membranes; 40% of this was specific binding, characterized by a plateau in serotonin antagonist inhibition curves, and another 40% was non-specific binding to structural recognition sites displaceable by unlabelled ketanserin. Specific [3H]ketanserin binding to platelets shows the features of serotonin S2-receptor binding sites previously identified in rat pre-frontal cortex and in striatum. In platelets, KD = 1.02 nM and Bmax = 86 fmol/10(9) platelets; the Ki values of 21 compounds were similar in the three different tissues.

摘要

[3H]酮色林与猫血小板膜有大量结合;其中40%为特异性结合,其特征是血清素拮抗剂抑制曲线呈平台期,另外40%为与未标记酮色林可置换的结构识别位点的非特异性结合。血小板上[3H]酮色林的特异性结合表现出先前在大鼠前额叶皮质和纹状体中鉴定出的血清素S2受体结合位点的特征。在血小板中,KD = 1.02 nM,Bmax = 86 fmol/10(9)个血小板;21种化合物的Ki值在三种不同组织中相似。

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