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２β－甲酯基－３β－（４－碘苯基）托烷（β－ＣＩＴ）与多巴胺转运蛋白（ＤＡＴ）、５－羟色胺转运蛋白（５－ＨＴＴ）亲和力几乎相等，因此可用５－ＨＴ重摄取抑制剂氯米帕明来研究５－ＨＴ系统与ＤＡ系统间的相互作用。用过氧乙酸氧化碘标记法制备~（１２５）Ｉ－β－ＣＩＴ。用不同剂量盐酸氯米帕明（０．２５、 ０．５、 １、 １．５、 ２、 ２．５ｍｇ）研究对~（１２５）Ｉ－β－ＣＩＴ脑内结合的影响，及同一剂量盐酸氯米帕明（１ｍｇ／０．４ｍＬ双蒸水）对~（１２５）Ｉ－β－ ＣＩＴ在脑内动态分布影响的结果表明：过氧乙酸氧化碘标记法标记率为５４．７０％±９．８１％，反应时间为２０－３０ｍｉｎ。ＨＰＬＣ及萃取分离纯化后的放化纯度（ＲＣＰ）为９９．３３％±０．１５％。不同剂量盐酸氯米帕明对~（１２５）Ｉ－β－ＣＩＴ脑内结合的影响：注射盐酸氯米帕明小鼠的脑干、海马、大脑额叶、顶叶、颞叶、枕叶皮质对~（１２５）Ｉ－β－ＣＩＴ摄取的％ＩＤ／ｇ、Ｔ／ＣＢ－１值均比对照组低，且含５－ＨＴＴ较多的区域的脑干、海马、额叶组织的％ＩＤ／ｇ与对照组有显著性差异（Ｐ＜０．０１）。纹状体区摄取~（１２５）２５１－β－ＣＩＴ的％ＩＤ／ｇ、 Ｔ／ＣＢ－１值均比对照组高。
The affinity of 2β-carbomethoxy-3β- (4-iodophenyl) tropane (β-CIT) to dopamine transporter (DAT) and serotonin transporter (5-HTT) Clomipramine, an inhibitor of uptake, was used to study the interaction between the 5-HT system and the DA system. Preparation of ~ (125) I-β-CIT with Peroxyl Acetate Iodide Labeling. The effect of clomipramine hydrochloride (0.25, 0.5, 1, 1.5, 2, 2.5 mg) on the intracerebral binding of ~ (125) I-β-CIT was studied with different doses of clomipramine hydrochloride and the same dose of hydrochloric acid The effect of clomipramine (1 mg / 0.4 mL double distilled water) on the dynamic distribution of 125 I-β-CIT in the brain showed that the labeling rate of iodated peroxynitrite iodine was 54.70% ± 9 .81%, the reaction time is 20-30min. The radiochemical purity (RCP) after HPLC and extraction separation and purification was 99.33% ± 0.15%. Effect of different doses of clomipramine on the intracerebral binding of ~ (125) I-β-CIT: The brain stem, hippocampus, frontal lobe, parietal lobe, temporal lobe, occipital cortex of clomipramine hydrochloride The% ID / g and T / CB-1 values of ~ (125) I-β-CIT were lower than that of the control group, and the% ID of brainstem, / G and the control group had significant difference (P <0.01). The% ID / g and T / CB-1 values of ~ (125) 251-β-CIT uptake in the striatum were higher than those in the control group.