Optimization of a convenient route to produce N-succinimidyl 4-radiodobenzoate for radioiodination of proteins.
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.
Araujo
E B
EB
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. ebaraujo@net.ipen.br
Santos
J S
JS
Colturato
M T
MT
Muramoto
E
E
Silva
C P G
CP
D002851:Chromatography, High Pressure Liquid / Q000379:methods; D007457:Iodine Radioisotopes / Q000737:chemistry* / Q000302:isolation & purification; D007463:Iodobenzoates / Q000138:chemical synthesis* / Q000737:chemistry / Q000302:isolation & purification; D007553:Isotope Labeling / Q000379:methods*; D008024:Ligands; D011506:Proteins / Q000138:chemical synthesis* / Q000737:chemistry / Q000302:isolation & purification; D011786:Quality Control; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000302:isolation & purification; D013696:Temperature
D007457:Iodine Radioisotopes; D007463:Iodobenzoates; D008024:Ligands; D011506:Proteins; D019275:Radiopharmaceuticals; C062338:N-succinimidyl 4-iodobenzoate