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Development of ^<99m>Tc-complexes for imaging cancer metastasis

用于癌症转移成像的^<99m>Tc复合物的开发

基本信息

批准号：
09672190
负责人：
NAKAYAMA Morio
金额：
$ 1.92万
依托单位：
Kumamoto University
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
1997
资助国家：
日本
起止时间：
1997 至 1998
项目状态：
已结题

来源：
https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-09672190/
关键词：
Hydroxamic acid Cancer ^<99m>Tc ヒドロキサムアミド ^<99m>Tc錯体

项目摘要

We planed to develope the imaging agent for cancer metastasis by the two approaches as followes :(1) Production of ^<99m>Tc-labded compounds by the introduction of ^<99m>Tc-complexes to the antibody or polypeptide that shows high affinity for the antigen or receptor on cell membrane of primary canncer and the importantfactor for angiogenesis(2) Development of ^<99m>Tc-coinplexes that show high affinity for tumor.Since ^<99m>Tc-iagnostic agents essetially contains the ^<99m>Tc by the coordinate bond, the behavior of ^<99m>Tc in vivo is very influenced by the equilibrium state involving the ligand and ^<99m>Tc. Accordingly, the present ^<99m>Tc-radiopharmaceuticals have developed on the base of the strategy described above (1), namely many researchers developed the various ligand systems that form the higly stable ^<99m>Tc-complexes. However, the ligand system availabe for the clinical use has not been completed.On the other hand, though it is known that seine polynucleus metal complexes show high affinity for tumor, the systematic research has never been carried out.In this study, We selected the two ligand systems to perform the duvelopment of ^<99m>Tc-complexes for imaging cancer metastasisboth by the two way. One is hydroxamamide ligand system which form stable ^<99m>Tc-complex. The other is hydroxamica acid ligand system which have the possibility for the formation of the polynucleous ^<99m>Tc-complexes. The difference in ligand system resulted in the change of the properties of ^<99m>Tc-complex and the behavior of ^<99m>Tc in vivo.

我们计划通过以下两种途径开发肿瘤转移显像剂：（1）<99m>通过将~（133）<99m>Tc-复合物引入对原发性肿瘤细胞膜上的抗原或受体具有高亲和力的抗体或多肽，以及血管生成的重要因素，来制备~（133）Tc-标记的化合物;（2）开发<99m>对肿瘤具有高亲和力<99m><99m><99m><99m>的~（133）Tc-复合物。因此，本发明的13 <99m>Tc-放射性药物是基于上述策略（1）开发的，即许多研究人员开发了形成高度稳定的13 Tc-复合物的各种配体系统<99m>。本研究选择这两种配体系统，分别<99m>用两种方法对~（13）Tc-配合物进行显像，并对~（13）Tc-配合物的显像效果进行了研究，结果表明，~（13）Tc-配合物的显像效果优于~（13）Tc-配合物。一种是异羟肟胺配体体系，形成稳定的<99m>Tc-络合物。另一种是异羟肟酸配体体系，该体系有可能形成多核~（13）<99m>Tc配合物。配体体系的不同导致了~（13）<99m>Tc-配合物性质的变化和~（13）<99m>Tc在体内的行为。