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Direct Labelling of Octreotide With 99Mtc: Effect of Different Concentration of Reducing Agents and Amount of Sodium Pertechnetate on Radiolabelling Efficiency Publisher Pubmed



Gandomkar M1 ; Najafi R1 ; Sadat Ebrahimi SE2 ; Shafiee A2 ; Babaei MH1 ; Rabbani M3 ; Shabani GA1
Authors
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Authors Affiliations
  1. 1. Radioisotope Division, Nuclear Research Center, Atomic Energy Organization of Iran, Tehran, Iran
  2. 2. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran Univ. of Medical Sciences, Tehran, Iran
  3. 3. Department of Pharmacology, Faculty of Pharmacy, Isfahan Univ. of Medical Sciences, Isfahan, Iran

Source: Applied Radiation and Isotopes Published:2003


Abstract

Octreotide, a synthetic analog of natural hormone somatostatin, was labelled with 99mTc. Labelling was accomplished by reduction of the cysteine bridge, which provided sulfhydryl groups for chelating with 99mTc. Sodium ascorbate and sodium dithionite in different concentrations were used as reducing agents. Different amounts of sodium pertechnetate were used for labelling of peptide. When the mass ratio of peptide and sodium ascorbate was 1:100 and the final concentration of dithionite in the labelling vial was 0.2-0.4μg/μl with 0.18-1.48GBq sodium pertechnetate more than 80% radiolabelling efficiency was confirmed by RP-HPLC, ITLC-SG and C18 Cartridge analysis. The stability of the 99mTc-peptide bond was evaluated by human serum challenge and that showed the stability was 90% after 4h. © 2003 Elsevier Science Ltd. All rights reserved.