Nuclear Science and Techniques

《核技术》(英文版) ISSN 1001-8042 CN 31-1559/TL     2019 Impact factor 1.556

Nuclear Science and Techniques ›› 2009, Vol. 20 ›› Issue (3): 163-169 doi: 10.13538/j.1001-8042/nst.20.163-169

• RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICIN • Previous Articles     Next Articles

Radiosynthesis and biodistribution of [18F]-tetracosactide using a semi-automated [18F]SFB production module

AKHLAGHI Mehdi1,* AHI Leyla Pashaye2 JALILIAN Amir Reza1 GAROUSI Javad1 POUR-HERAVI Mohammad Reza Abdolrahim2   

  1. 1Nuclear Medicine Group, Agriculture, Medicine and Industrial Research School, Karaj, Iran 2Chemistry Department, Payame Noor University of Abhar, Abhar, Iran
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AKHLAGHI Mehdi, AHI Leyla Pashaye, JALILIAN Amir Reza, GAROUSI Javad. Radiosynthesis and biodistribution of [18F]-tetracosactide using a semi-automated [18F]SFB production module.Nuclear Science and Techniques, 2009, 20(3): 163-169     doi: 10.13538/j.1001-8042/nst.20.163-169

Abstract:

In order to prepare a specific melanocortin type 2 receptor (MC2R) ligand, ?1-24-corticotrophin was prepared in one-step reaction with [18F] SFB and ?-1-24-corticotrophin pharmaceutical solution (1 mg/mL, pH=6.5). [18F]SFB was prepared in a semi-automated module in two steps with an overall radiochemical yield of 47% to EOB (not-decay corrected) in 90 min. The 18F-labeled intermediates and 18F-labeled peptide was checked by RTLC and HPLC. The results show that the radiochemical purity is >95% and the yield to EOB (not-decay corrected) is 29% for final 18F-labeled peptide at optimized conditions. Preliminary in vivo studies in normal mice were performed to determine biodistribution of the 18F-labeled peptide for 150 min. The results show that the major tracer uptake is consistent with the natural distribution of MC2R receptors in mammals. Testes/blood and testes/muscle ratios for 18F-labeled peptide at 150 min were 184 and 1.56, respectively, and adipocyte/blood and adipocyte/muscle ratios at 120 min were 221 and 142, respectively. The data support the specific receptor binding of the radiolabeled peptide as reported for MC2R receptor accumulation in adipocytes and testes and demonstrates the retention of biological activity of the peptide. This tracer can be used in detection of MC2R distribution in malignancies and sex organ diseases.

Key words: Mc2r, beta-1-24-corticotrophin, Fluorine-18, Radiolabeling, Biodistribution