Wilbur D S, Hadley S W, Grant L M, Hylarides M D
NeoRx Corporation, Seattle, Washington 98119.
Bioconjug Chem. 1991 Mar-Apr;2(2):111-6. doi: 10.1021/bc00008a006.
A comparative investigation of the biodistributions of radioiodinated p- and m-iodobenzoyl conjugates of a monoclonal antibody Fab fragment, NR-LU-10 Fab, and the same antibody Fab fragment radioiodinated by the chloramine-T (ChT) method has been carried out in mice. Coinjected, dual-isotope studies in athymic mice with tumor xenografts have demonstrated that there are only minor differences in the in vivo distributions of the iodobenzoyl-labeled Fabs, except in the excretory organs, kidneys, and intestines, where major differences were observed. Similarly, coinjection of either the p-iodobenzoyl or m-iodobenzoyl conjugate of NR-LU-10 Fab with the Fab radioiodinated with ChT/radioiodide into BALB/c mice provided additional data that indicated that the two iodobenzoyl conjugates distributed similar in a number of selected tissues. The tissue-distribution differences of the regioisomeric iodobenzoyl conjugates in relation to the ChT-radioiodinated Fab were large for the stomach and neck, consistent with previous studies. The most notable difference between the two iodobenzoyl conjugates was the kidney activity, where the m-iodobenzoyl conjugate was similar to the directly labeled Fab, but the p-iodobenzoyl-conjugated Fab was higher by nearly a factor of 2.
已在小鼠体内对单克隆抗体Fab片段NR-LU-10 Fab的对碘苯甲酰和间碘苯甲酰缀合物的放射性分布，以及通过氯胺-T（ChT）法放射性碘化的相同抗体Fab片段进行了比较研究。在患有肿瘤异种移植的无胸腺小鼠中进行的共注射双同位素研究表明，除了在排泄器官、肾脏和肠道中观察到主要差异外，碘苯甲酰标记的Fabs在体内分布仅有微小差异。同样，将NR-LU-10 Fab的对碘苯甲酰或间碘苯甲酰缀合物与用ChT/放射性碘碘化的Fab共注射到BALB/c小鼠中，提供了额外数据，表明两种碘苯甲酰缀合物在许多选定组织中的分布相似。对于胃和颈部，区域异构碘苯甲酰缀合物与ChT放射性碘化的Fab之间的组织分布差异很大，这与先前的研究一致。两种碘苯甲酰缀合物之间最显著的差异是肾脏活性，其中间碘苯甲酰缀合物与直接标记的Fab相似，但对碘苯甲酰缀合的Fab高出近2倍。
