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作 者:刘飞[1] 李洪玉[2] 梁积新[2] 刘英妹[2] 贺佑丰[2] 罗志福[2] 王荣福[3] 何晓坤[3] 张春丽[3] 付占立[3]
机构地区:[1]北京师范大学化学系,100875 [2]中国原子能科学研究院同位素研究所,北京102413 [3]北京大学第一医院核医学科
出 处:《中华核医学杂志》2003年第2期110-113,共4页Chinese Journal of Nuclear Medicine
基 金:国际原子能机构 (IAEA)基金资助项目 (91 0 4 R)
摘 要:目的 探讨研制99Tcm [N (2 (4 (2 甲氧基苯 ) 1 哌嗪 1 乙基 ) N (2 吡啶 ) 环己烷酰胺 ) ](WAY10 0 6 35 )类似物中枢神经系统 5 羟色胺 1A(5 HT1A)受体显像剂。方法 将化学合成的单齿配体 1 (2 甲氧基苯基 ) 4 (2 巯基乙基 )哌嗪 (MPMEP)和三齿配基N ,N 二 (2 巯基乙基 ) N′,N′ 二乙基乙二胺 (BMPDEEDA)与99Tcm 葡庚糖酸钠 (GH)经三齿配体与单齿配体混合标记方法 (“3+1”)混合配体交换 ,制得99TcmO(MPMEP) (BMPDEEDA)。同时 ,以大鼠脑海马膜组织匀浆为 5 HT1A 受体来源 ,与 5 HT1A受体的特异激动剂3H 2 (二 n 丙胺基 ) 8 羟基 四氢化萘 (8 OH DPAT)进行体外竞争结合实验 ,测定99Tcm 标记物的类似物ReO(MPMEP) (BMPDEEDA)对受体蛋白与特异拮抗 (激动 )剂竞争结合达到一半 (5 0 % )时的浓度 (IC50 值 )。结果 制备的99TcmO(MPMEP) (BMPDEEDA)经高压液相层析 (HPLC)纯化并测定其放化纯度 >95 %。大鼠脑海马摄取在注射后 30、6 0、12 0、180min时 %ID g分别为 0 .0 77、0 .0 6 8、0 .0 84和 0 .0 6 7,放射性摄取最高部位为丘脑 ,注射后 12 0min时 %ID g为 0 .15 4 ,各时相海马与小脑的摄取比值分别为 0 .84 7、0 .880、0 .92 1和 1.2 4 4。ReO(MPMEP) (BMPDEEDA)的IC50为 98.Objective To investigate 99 Tc m labeled analog of WAY100635 as potential serotonin 5 hydroxytryptamine 1A (5 HT 1A ) receptor imaging agent. Methods 99 Tc mO(MPMEP)(BMPDEEDA) was prepared by '3+1' mixed ligand approach using monodentate ligand 1 (2 methoxyphenyl) 4 (2 mercaptoethyl)piperazine (MPMEP), tridentate ligand N,N bis(2 mercaptoethyl) N′,N′ diethylethylenediamine (BMPDEEDA) and 99 Tc m glucoheptonate (GH). Animal studies were performed in Wistar rats and normal mice. The analogous Re complex was synthesized as a surrogate for the 99 Tc m complex for using in receptor binding assays. Re complex was tested with in vitro competition binding assays against 3H 8 OH DPAT. Results Radiochemical purity of 99 Tc mO (MPMEP)(BMPDEEDA) was over 95% after purification by HPLC. The regional distribution in Wistar rat brain showed that hippocampus uptakes were 0.077, 0.068, 0.084 and 0.067%ID/g at 30, 60, 120 and 180 min postinjection, respectively. The ratios of hippocampus uptake to cerebellar uptake were 0.847, 0 880, 0.921 and 1.244 at 30, 60, 120 and 180 min postinjection, respectively. IC 50 value of ReO(MPMEP)(BMPDEEDA) was 98.7 nmol/L. Conclusion The results of this study demonstrate that 99 Tc mO(MPMEP) (BMPDEEDA) as a serotonin 5 HT 1A receptor imaging agent is worthy of further investigation.
关 键 词:5-HTlA 受体显像剂 ^99Tc^mO(MPMEP) 5-羟色胺 化学合成
分 类 号:R817.9[医药卫生—影像医学与核医学]
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