Wilbur D S, Hadley S W, Hylarides M D, Abrams P G, Beaumier P A, Morgan A C, Reno J M, Fritzberg A R
NeoRx Corporation, Seattle, WA 98119.
J Nucl Med. 1989 Feb;30(2):216-26.
A method of radioiodinating monoclonal antibodies such that the labeled antibodies do not undergo in vivo deiodination has been studied. The method utilizes conjugation of succinimidyl para-iodobenzoate to the antibody. The iodobenzoate was radiolabeled by using an organometallic intermediate to facilitate the reaction. Thus, succinimidyl para-tri-n-butylstannylbenzoate was radiolabeled in 60-90% radiochemical yield and subsequently conjugated to the antibody in 80-90% yield. Animal biodistribution studies were carried out with two separate anti-melanoma antibodies (9.2.27 and NR-M1-05) labeled by this method, and examined in nude mice bearing human melanoma tumor xenografts. Very large differences in the localization of radioactivity were observed in the thyroids and stomachs of mice when the iodobenzoyl-labeled antibodies were compared with the same antibodies labeled using the chloramine-T method of radioiodination. Few other significant differences in the tissue distribution of the radioiodinated antibodies were seen.
一种对单克隆抗体进行放射性碘化的方法已被研究，该方法能使标记后的抗体在体内不发生脱碘。该方法利用对碘苯甲酸琥珀酰亚胺酯与抗体进行偶联。通过使用有机金属中间体促进反应，对碘苯甲酸酯被放射性标记。因此，对三正丁基锡苯甲酸琥珀酰亚胺酯的放射性标记产率为60 - 90%，随后与抗体偶联的产率为80 - 90%。用这种方法标记的两种不同的抗黑色素瘤抗体（9.2.2 和NR - M1 - 05）进行了动物体内生物分布研究，并在携带人黑色素瘤肿瘤异种移植的裸鼠中进行了检测。当将碘苯甲酰标记的抗体与使用氯胺 - T放射性碘化方法标记的相同抗体进行比较时，在小鼠的甲状腺和胃中观察到放射性定位存在非常大的差异。在放射性碘化抗体的组织分布中几乎没有看到其他显著差异。
