中华核医学杂志
中華覈醫學雜誌
중화핵의학잡지
CHINESE JOURNAL OF NUCLEAR MEDICINE
2008年
4期
223-226
,共4页
杨敏%徐宇平%潘栋辉%王颂佩%唐婕%黄洪波%罗世能
楊敏%徐宇平%潘棟輝%王頌珮%唐婕%黃洪波%囉世能
양민%서우평%반동휘%왕송패%당첩%황홍파%라세능
Fallypride%化学合成%自动化%氟放射性同位素%受体,多巴胺%体层摄影术,发射型计算机%小鼠
Fallypride%化學閤成%自動化%氟放射性同位素%受體,多巴胺%體層攝影術,髮射型計算機%小鼠
Fallypride%화학합성%자동화%불방사성동위소%수체,다파알%체층섭영술,발사형계산궤%소서
Fallypride%Chemical synthesis%Automation%Fluorine radioisotopes%Receptors,dopamine%Tomography,emission-computed%Mice
目的 研究高效、简单的自动化合成多巴胺D2受体显像剂(S)-(-)-N-(1-烯丙基吡咯烷-2-氨基甲基)-5-(3-18F)-2,3-二甲氧基苯甲酰胺(18F-Fallypride)的方法,并用小动物PET观察其在小鼠活体内的生物分布.方法 采用国产氟标记多功能模块控制整个过程,18F-在乙腈溶液中与前体(s)-(-)-N-(1-烯丙基吡咯烷-2-氨基甲基)-5-(3-磺酰基)-2,3-二甲氧基苯甲酰胺(OTSF)直接反应生成18F-Fallypride,混合物装柱,产品被C18柱吸附,用水冲洗柱,用少量乙醇淋出,加生理盐水稀释.ICR小鼠给药后经小动物PET活体显像.结果 18F-Fallypride放化产率为40.7%(已校正),合成时间为40 min,无需高效液相色谱(HPLC)法分离,放化纯＞95%.注射18F-Fallypride后ICR小鼠经小动物PET显像,脑内纹状体区域摄取最高,且双侧放射性浓聚对称,清除较慢.结论 18F-Fallypride自动化合成速度快,效率高.18F-Fallypride适于多巴胺D2受体显像.
目的 研究高效、簡單的自動化閤成多巴胺D2受體顯像劑(S)-(-)-N-(1-烯丙基吡咯烷-2-氨基甲基)-5-(3-18F)-2,3-二甲氧基苯甲酰胺(18F-Fallypride)的方法,併用小動物PET觀察其在小鼠活體內的生物分佈.方法 採用國產氟標記多功能模塊控製整箇過程,18F-在乙腈溶液中與前體(s)-(-)-N-(1-烯丙基吡咯烷-2-氨基甲基)-5-(3-磺酰基)-2,3-二甲氧基苯甲酰胺(OTSF)直接反應生成18F-Fallypride,混閤物裝柱,產品被C18柱吸附,用水遲洗柱,用少量乙醇淋齣,加生理鹽水稀釋.ICR小鼠給藥後經小動物PET活體顯像.結果 18F-Fallypride放化產率為40.7%(已校正),閤成時間為40 min,無需高效液相色譜(HPLC)法分離,放化純＞95%.註射18F-Fallypride後ICR小鼠經小動物PET顯像,腦內紋狀體區域攝取最高,且雙側放射性濃聚對稱,清除較慢.結論 18F-Fallypride自動化閤成速度快,效率高.18F-Fallypride適于多巴胺D2受體顯像.
목적 연구고효、간단적자동화합성다파알D2수체현상제(S)-(-)-N-(1-희병기필각완-2-안기갑기)-5-(3-18F)-2,3-이갑양기분갑선알(18F-Fallypride)적방법,병용소동물PET관찰기재소서활체내적생물분포.방법 채용국산불표기다공능모괴공제정개과정,18F-재을정용액중여전체(s)-(-)-N-(1-희병기필각완-2-안기갑기)-5-(3-광선기)-2,3-이갑양기분갑선알(OTSF)직접반응생성18F-Fallypride,혼합물장주,산품피C18주흡부,용수충세주,용소량을순림출,가생리염수희석.ICR소서급약후경소동물PET활체현상.결과 18F-Fallypride방화산솔위40.7%(이교정),합성시간위40 min,무수고효액상색보(HPLC)법분리,방화순＞95%.주사18F-Fallypride후ICR소서경소동물PET현상,뇌내문상체구역섭취최고,차쌍측방사성농취대칭,청제교만.결론 18F-Fallypride자동화합성속도쾌,효솔고.18F-Fallypride괄우다파알D2수체현상.
Objective Benzamide,5-(3-fluoropropyl)-2,3-dimethoxy-N-[(2S)-1-(2-propenyl)-2-pyrrolidinyl]methyl(Fallypride)is a well-known dopamine D2 and D3 antagonist.18F-Fallypride PET has been used to study D2 and D3 receptor occupancy and density in neuropsychiatric disorders and aging in humans.This study aimed to develop an automated synthesis of the potent dopamine D2 and D3 receptor PET imaging agent and to study the distribution of the mice by small-animal PET.Methods 18F ion Was reacted with precursor(s)-(-)-N-(1-allyl-2-pyrrolidinyl)methyl-5-(3-tolunesulfonyloxypropyl)-2,3-dimethoxy-benzamide in a chemical process control unit(CPCU).The crude product was transported to a C18 column.18F-Fallypride was absorbed on the column.the column Was washed by water.18F-Fallypride was then eluted from the column with small volume of ethanol.The mice were imaged by small-animal PET after in travenous 18F-Fallypride(1.85 MBq).Results It took 40 min for synthesizing 18F-Fallypride at CPCU,the radiochemical yield was 40.7%(end of synthesis),and the radiochemistry purity Was over 95%.Higher accumulation and delayed clearance of the 18F-Fallypride at bilateral striata was noted in imaging mouse brain with small-animal PET.Conclusions An optimal yielding of 18F-Fallypride at CPCU could be obtained.18F-Fallypride could demonstrate dopamine D2 and D3 receptor at mouse brain.
