Uptake　of　^(99m)Tc^(5+)-complexes　in　ischemic　myocardial　slices　and　theirdisociable　ability  

Uptake of 99m Tc 5+ complexes in ischemic myocardial slices and their dissociable ability

作　　者：李少林[1] 颜学先[1] 刘孝云[1] 

机构地区：[1]重庆医科大学实验核医学教研室

出　　处：《中国药理学报》1997年第5期465-467,共3页Acta Pharmacologica Sinica

摘　　要：目的：研究在机体内具有一定的稳定性而又能离解出可到达靶组织的活性形式ＴｃＯ３－４的多核锝标记化合物．方法：模仿锝标记化合物进入血循环后的状况，采用稀释的方法，用硅胶板薄层层析法来测量其离解能力的大小．结果：５００倍稀释液的离解物峰的相对放射性百分数为：９９ｍＴｃ５＋ｓｕｃｉｍｅｒ为０，９９ｍＴｃ５＋ＧＨ为２８１％±１３％，９９ｍＴｃ５＋ＰＰｉ为４６０％±２９％，而缺血３ｈ的心肌中的摄取为：９９ｍＴｃ５＋ｓｕｃｉｍｅｒ是４２０％±１１０％ｄｏｓｅ／ｇｔｉｓｕｅ，９９ｍＴｃ５＋ＧＨ是７１０％±１８０％ｄｏｓｅ／ｇｔｉｓｕｅ，９９ｍＴｃ５＋ＰＰｉ是１２９５％±３９０％ｄｏｓｅ／ｇｔｉｓｕｅ．结论：以上几种多核螯合物的离解性与其在缺血性心肌中的摄取成正相关关系．AIM: To find how some technetium complexes to deliver the active species, TcO 3- 4, to the target tissue from a dissociable polynuclear Tc 5+ species in preserved states in vivo . METHODS: Effect of dissociation ability of the polynuclear Tc 5+ complexes on their accumulation in ischemic myocardium was tested. Ability of dissociation as having an appropriate conformation to become biologically functional after entering the blood circulation was tested using a simple dilution method by thin layer chromatography (TLC) analysis. Various degree of ischemic myocardium slices of rat were incubated with 1/100 diluted 99m Tc 5+ succimer , 99m Tc 5+ GH and 99m Tc 5+ PPi . RESULTS: The TLC patterns of 99m Tc 5+ GH and 99m Tc 5+ PPi showed the presence of a fast increasing of free Tc species as dilution degree increased. The relative radioactivity of peak of free pertechnetate ( R f=0 85-1 0) with 1∶500 dilution was: 99m Tc 5+ succimer 0 % , 99m Tc 5+ -GH 28 1 % ±1 3 % , and 99m Tc 5+ PPi 46 0 % ±2 9 % respectively. The uptake of the myocardium after ischemia for 3 h was 99m Tc 5+ succimer 420 % ±110 % dose/g tissue, 99m Tc 5+ GH 710 % ±180 % dose/g tissue, and 99m Tc 5+ PPi 1295 % ±390 % dose/g tissue respectively. CONCLUSION: The dissociation and myocardial uptake showed: 99m Tc 5+ succimer < 99m Tc 5+ GH < 99m Tc 5+ PPi , the uptake by the ischemic myocardium is positively correlated to their dissociation.

关 键 词：药物稳定性 心肌缺血 锝^99M 

分 类 号：R542.205[医药卫生—心血管疾病]