Shiba K, Mori H, Matsuda H, Hisada K
Radioisotope Center, School of Medicine, Kanazawa University, Japan.
Nucl Med Commun. 1991 Dec;12(12):1057-65. doi: 10.1097/00006231-199112000-00007.
In an effort to develop new, clinically useful 99Tcm-diaminodithiol (99Tcm-DADT) complexes for the evaluation of regional cerebral perfusion, basic diaminodithiols (DADT-TM, DADT-HM and DADT-MHM) and three diaminodithiol ligands functionalized with p-iodophenethyl (DADT-IPE), N-ethyl-p-fluorophenethyl amine (DADT-EFPE) or N-ethyl-p-iodophenethyl amine (DADT-EIPE), whose chemical structures are analogous to N-isopropyl-p-iodoamphetamine (IMP), were synthesized, labelled with 99Tcm and evaluated comparatively in experimental animals. In addition, the relationships between the chemical properties of the derivatives and their brain uptake and retention were investigated. The results were: (1) Isomeric configuration of 99Tcm-DADT complexes has an influence on uptake and retention in the rat brain. (2) In basic 99Tcm-DADT complexes, a correlation exists between initial brain uptake and lipophilicity, but in 99Tcm-DADT complexes containing a chemical structure similar to that of IMP, no correlation exists. (3) 99Tcm-DADT-IPE has relatively high uptake and long retention in the rat brain.
为了开发用于评估局部脑灌注的新型临床可用99锝-二氨基二硫醇（99Tcm-DADT）配合物，合成了碱性二氨基二硫醇（DADT-TM、DADT-HM和DADT-MHM）以及三种用对碘苯乙基（DADT-IPE）、N-乙基对氟苯乙胺（DADT-EFPE）或N-乙基对碘苯乙胺（DADT-EIPE）官能化的二氨基二硫醇配体，其化学结构类似于N-异丙基对碘安非他明（IMP），用99Tcm进行标记，并在实验动物中进行比较评估。此外，还研究了衍生物的化学性质与其脑摄取和滞留之间的关系。结果如下：（1）99Tcm-DADT配合物的异构体构型对大鼠脑中的摄取和滞留有影响。（2）在碱性99Tcm-DADT配合物中，初始脑摄取与亲脂性之间存在相关性，但在含有与IMP化学结构相似的99Tcm-DADT配合物中，不存在相关性。（3）99Tcm-DADT-IPE在大鼠脑中具有相对较高的摄取和较长的滞留时间。
