^(99m)Tc(CO)_3-CHIPDTC配合物的制备及其生物分布

PREPARATION AND BIODISTRIBUTION OF ^(99m)Tc(CO)_3-CHIPDTC COMPLEX IN MICE

采用fac-9[9mTc(CO)3(H2O)3]+与N-环己基-N-异丙基-氨荒酸盐(CHIPDTC)在室温下发生配体交换反应制得99mTc(CO)3-CHIPDTC配合物.用薄层层析(TLC)法和高效液相色谱(HPLC)法鉴定该配合物的放射化学纯度大于90%.该配合物是一种体外稳定性良好的脂溶性电中性物质.99mTc(CO)3-CHIPDTC配合物在小鼠体内生物分布结果表明,其心、脑摄取值偏低,有待进一步结构修饰以获取新型优良放射性药物.

Organometallic precursor fac-[99mTc（CO）3（H2O）3]＋ was reacted with N-cyclohexyl N-isopropyl dithiocarbamate（CHIPDTC） at room temperature to produce 99mTc（CO）3-CHIPDTC complex,with the product being over 90% radiochemically pure（RCP） as measured by thin layer chromatography（TLC） and high performance liquid chromatography（HPLC）.The resultant complex was neutral,lipophilic and stable for over 6 hrs at room temperature.Biodistribution studies of 99mTc（CO）3-CHIPDTC and 99mTcN-CHIPDTC complexes in mice indicated that the 9mTc（CO）3 complex showed a much lower uptake in brain and heart.It is concluded that to obtain a suitable radiopharmaceutical,structure of the dithiocarbamate ligand should be modified structurally in the future.