用于蛋白质放射性碘化的N-琥珀酰亚胺基-4-放射性苯甲酸酯便捷合成路线的优化。

Optimization of a convenient route to produce N-succinimidyl 4-radiodobenzoate for radioiodination of proteins.

作者信息

Araujo E B, Santos J S, Colturato M T, Muramoto E, Silva C P G

机构信息

Centro de Radiofarmácia do Instituto de Pesquisas Energéticas e Nucleares, IPEN-CNEN/SP, Rua do Lago, Travessa R 400, Cidade Universitária, São Paulo, CEP 05508-900, Brazil.

出版信息

Appl Radiat Isot. 2003 Jun;58(6):667-73. doi: 10.1016/s0969-8043(03)00068-x.

DOI:10.1016/s0969-8043(03)00068-x

PMID:12798375

Abstract

The preparation of N-succinimidyl-4-[131I]iodobenzoate (SIB) has been optimized using an alternative technique employing Cu(I)-assisted radioiododebromination that produces p-[131I]iodobenzoic acid. The reaction conditions were optimized and radiochemical purity of more than 90% was obtained when using 160 degrees C, 60 min reaction time and a [CuCl]/[p-bromobenzoic acid] relation of about 10(-2). After purification, the p-[131I]iodobenzoic acid reacted with TSTU to produce the SIB in a radiochemical yield greater than 98%. Protein conjugation using SIB resulted in a relatively low radiochemical yield. Biological distribution studies evidenced the in vivo stability of the labeled protein.

摘要

已使用一种替代技术优化了N-琥珀酰亚胺基-4-[¹³¹I]碘苯甲酸酯（SIB）的制备，该技术采用铜（I）辅助的放射性碘脱溴反应来生成对-[¹³¹I]碘苯甲酸。优化了反应条件，当使用160℃、60分钟反应时间和约10⁻²的[CuCl]/[对溴苯甲酸]比例时，获得了超过90%的放射化学纯度。纯化后，对-[¹³¹I]碘苯甲酸与TSTU反应生成SIB，放射化学产率大于98%。使用SIB进行蛋白质偶联导致放射化学产率相对较低。生物分布研究证明了标记蛋白在体内的稳定性。