Chan B, Madras B K
Eur J Pharmacol. 1983 Mar 4;87(4):357-65. doi: 10.1016/0014-2999(83)90074-2.
Frontal cortex membranes were solubilized with digitonin, prelabelled with 4 nM [3H]mianserin, and partially purified by isoelectric focussing. Bound [3H]mianserin separated from free [3H]mianserin as a single radioactive peak with a pI value of 5.03. A 14-fold purification was achieved. Focussing in the presence of 1 microM ketanserin (R 41468) or 1 microM chlorpyramine (a histamine H1-antagonist) or 10 microM spiperone (an S2-antagonist) completely abolished the peak of radioactivity at pH 5. Pharmacological characterization of the eluted radioactive peak revealed both histaminergic and serotonergic binding properties. The data suggest that the serotonergic and histaminergic components of [3H]mianserin binding to frontal cortex are not separable by solubilization, gel filtration or isoelectric focussing.
用洋地黄皂苷溶解额叶皮质膜，用4 nM [3H]米安色林进行预标记，并通过等电聚焦进行部分纯化。结合的[3H]米安色林与游离的[3H]米安色林分离，形成一个单一的放射性峰，其pI值为5.03。实现了14倍的纯化。在存在1 microM酮色林（R 41468）或1 microM氯苯那敏（一种组胺H1拮抗剂）或10 microM螺哌隆（一种S2拮抗剂）的情况下进行聚焦，完全消除了pH 5时的放射性峰。对洗脱的放射性峰进行药理学表征，揭示了组胺能和5-羟色胺能结合特性。数据表明，[3H]米安色林与额叶皮质结合的5-羟色胺能和组胺能成分不能通过溶解、凝胶过滤或等电聚焦分离。
