Abstract
本研究合成一系列乙烯亞胺酚四芽配位子 En(IP)2 [ethylene imine phenol]、MEn(IP)2 [methylethylene imine phenol]、DEn(IP)2 [dimethylethylene imine phenol]、Ch(IP)2 [cyclohexylethylene imine phenol]，以 99mTcO4- 之生理食鹽水溶液及 SnCl2 還原劑，經適 當步驟得鎝99m標幟乙烯亞胺酚化合物[99mTcLO]+ ( L為乙烯亞胺酚配位 子, O為氧)，進而以P(CH3)3(簡稱 Pm)、P(OCH3)3(簡稱 Pom) 或 P(OC2 H5)3 (簡稱 Poe)單芽配位子，還原並配位結合鎝99m乙烯亞胺酚化合物成 帶正一價具親脂性之鎝99m乙烯亞胺酚-膦化合物[99mTcLY2]+ (Y為三級膦 配位子)其化性以溶劑萃取法、電泳動分析法、高效益液相層析法予以分 析測知其標幟效率、親脂性、電性、穩定度等重要參數，藉以尋找出可應 用於核醫心臟造影之放射性鎝99m標幟化合物。經分析結果發現在所有合 成鎝99m乙烯亞胺酚-膦化合物中，[99mTc-DEn(IP)2-Pom]+ 所具有的標幟 效率、親脂性、正一價電性及穩定度，最符合心臟造影劑的要求。進一步 在大白鼠生物分佈試驗中，此鎝99m標幟化合物也顯現一高度心肌攝入量( ~ 16.21 %cpm/g)，且經 3 小時內仍穩定滯留，頗具發展為未來臨床核醫 心肌灌注診斷造影劑之潛力。 In this study, a series of ethylene imine phenol ligands,En( IP)2 [ethylene imine phenol],MEn(IP)2 [methylene imine phenol], DEn(IP)2 [dimethylethyl- ene imine phenol], Ch(IP)2 [cyclohexylethylene im- ine phenol] were synthesized. By means of mixing 99mTcO4- saline solution and SnCl2/ethanol solut- ion with the imine phenol ligands and heating at 95 oC for 15 min, a serial 99mTc labeled imine phenol complex [99mTcLO]+ were formed, where L re- presents the ethylene imine phenol ligands. Subsequently, phosphine or phosphite compound, P(CH3)3,P(OCH3)3 or P(OC2H5)3 was added and heated at 50oC for 45 min to reduce the technetium in the previously formed 99mTc coordinated ethylene imine phenols from Tc(V) to Tc(III). A stable mono- cationic and lipophilic 99mTc labeled phosphine ethylene imine phenol compound [99mTcLY2]+ (Y re- presents the phosphine or phosphite compound)would be obtained by the procedure.The chemical charact- eristics of the [99mTcLO]+ or [99mTcLY2]+ complexes were asseyed by solvent extraction, electrophoresis and high performance liquid chromatography.Labeling efficiency, lipophilicity,electrical charge and sat- bility of each of the [99mTcLY2]+ complexes were obtained from the analytical results. Among these 99mTc labeled complexes,[99mTc-DEn(IP) 2-Pom]+ shows the most promising chemical property as myocardial imaging agent. Rat biodistribution study of this complex also reveals a high myocard- ium uptake (~16.21 %cpm/g) and a stable retention in 3 hr. It is concluded from the study that [99m Tc-DEn(IP)2-Pom]+ exhibits the potential to be furthermore evaluated as a clinical myocardial perfusion agent.