Clelland C C, Giles K D, Farley T D, Gee Q, Wright J R
Physiol Chem Phys Med NMR. 1986;18(1):37-40.
The 64Cu-radiolabeled mixed valence cluster ion of copper and penicillamine (Cu(I)8Cu(II)6Pen12Cl5-) is easily prepared and purified in a 30 minute procedure. Mice were dosed intravenously with this substance at 0.1 mg/kg, and the distribution of the isotope among organs and tissues was quantified by gamma scintillometry of the isotope's positron annihilation radiation. The largest concentration was found in urine (a 96-fold increase over whole body specific activity at 20 minutes), and this finding is consistent with the compound's inulin-like renal clearance. Isotope levels were also elevated in kidney and liver tissues (2.36-and 3.62-fold, respectively), while all other organs and tissues examined were found to be depleted of the label. A pre-injection of unlabeled cluster at 60 mg/kg effectively blocked radiolabel interaction with liver tissue. This intensely red-violet compound did not stain viable liver cells, and it was not significantly decomposed by liver homogenates over a three hour period. These results suggest cluster interaction at saturable binding sites on liver cell surfaces. The unlabeled cluster shows no indication of toxicity, and the labeled version might have biomedical applications.
铜与青霉胺的64Cu放射性标记混合价簇离子（Cu(I)8Cu(II)6Pen12Cl5-）可在30分钟的流程内轻松制备并纯化。以0.1mg/kg的剂量给小鼠静脉注射该物质，通过对该同位素正电子湮灭辐射进行γ闪烁扫描法来定量同位素在各器官和组织中的分布。在尿液中发现了最高浓度（在20分钟时比全身比活度高96倍），这一发现与该化合物类菊粉样的肾脏清除情况相符。肾脏和肝脏组织中的同位素水平也有所升高（分别为2.36倍和3.62倍），而所检查的所有其他器官和组织中的标记物均减少。以60mg/kg的剂量预先注射未标记的簇合物可有效阻断放射性标记物与肝脏组织的相互作用。这种深红色紫色化合物不会对活的肝细胞染色，并且在三小时内不会被肝脏匀浆显著分解。这些结果表明簇合物在肝细胞表面的可饱和结合位点上发生相互作用。未标记的簇合物未显示出毒性迹象，而标记版本可能具有生物医学应用。
