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

Mehdi AKHLAGHI; Leyla Pashaye AHI; Amir Reza JALILIAN; Javad GAROUSI; Mohammad Reza Abdolrahim POUR-HERAVI

doi:10.13538/j.1001-8042/nst.20.163-169

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

RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE | Updated：2021-01-29

- Radiosynthesis and biodistribution of [¹⁸F]-tetracosactide using a semi-automated [¹⁸F]SFB production module
- Nuclear Science and Techniques Vol. 20, Issue 3, (2009)
- Affiliations：
  
  1.Nuclear Medicine Group, Agriculture, Medicine and Industrial Research School, Karaj, Iran
  2.Chemistry Department, Payame Noor University of Abhar, Abhar, Iran
- Author bio：
  
  Corresponding author. E-mail address: Makhlaghi@nrcam.org
  
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- DOI：10.13538/j.1001-8042/nst.20.163-169 CLC：
- Published：20 June 2009，
  
  Received：06 March 2009，
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Cite this article
Mehdi AKHLAGHI, Leyla Pashaye AHI, Amir Reza JALILIAN, et al. Radiosynthesis and biodistribution of [¹⁸F]-tetracosactide using a semi-automated [¹⁸F]SFB production module. [J]. Nuclear Science and Techniques 20(3):163-169(2009)
DOI：

Mehdi AKHLAGHI, Leyla Pashaye AHI, Amir Reza JALILIAN, et al. Radiosynthesis and biodistribution of [¹⁸F]-tetracosactide using a semi-automated [¹⁸F]SFB production module. [J]. Nuclear Science and Techniques 20(3):163-169(2009) DOI： 10.13538/j.1001-8042/nst.20.163-169.

Radiosynthesis and biodistribution of [ 18 F]-tetracosactide using a semi-automated [ 18 F]SFB production module 1 corresp first-author Corresponding author. E-mail address: Makhlaghi@nrcam.org Corresponding author. E-mail address: Makhlaghi@nrcam.org Makhlaghi@nrcam.org 2 1 1 2 Nuclear Medicine Group, Agriculture, Medicine and Industrial Research School, Karaj, Iran Nuclear Medicine Group, Agriculture, Medicine and Industrial Research School, Karaj, Iran Chemistry Department, Payame Noor University of Abhar, Abhar, Iran Chemistry Department, Payame Noor University of Abhar, Abhar, Iran In order to prepare a specific melanocortin type 2 receptor (MC2R) ligand, β 1-24 -corticotrophin was prepared in one-step reaction with [ 18 F] SFB and β-1-24-corticotrophin pharmaceutical solution (1 mg/mL, pH=6.5). [ 18 F]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 18 F-labeled intermediates and 18 F-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 18 F-labeled peptide at optimized conditions. Preliminary in vivo studies in normal mice were performed to determine biodistribution of the 18 F-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 18 F-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. Mc2r β-1-24-corticotrophin Fluorine-18 Radiolabeling Biodistribution References Cone R D , Mountjoy K G , Trends Endocrin Met , 1993 , 4 ( 7 ): 242 - 247 . Trends Endocrin Met Mountjoy K G , Robbins L S , Mortrud M T , et al . Science , 1992 , 257 ( 5074 ): 1248 - 1251 . Science Baxter J D , Tyrrel J D , the Adrenal Cortex . In: Felig P , Baxter J D , Broadus A E , et al . eds. Endocrinology and Metabolism . 2 nd Ed. New York : McGraw-Hill , 1986 : 511 - 692 . the Adrenal Cortex Slominski A , Ermak G , Mihm M . J Clin Endocrinol Metabol , 1996 , 81 ( 7 ): 2746 - 2749 . J Clin Endocrinol Metabol Lin C J , Alexander A A J , Latronico A C , et al . J Clin Endocrinol Metabol , 2000 , 85 ( 3 ): 1211 - 1214 . J Clin Endocrinol Metabol Boston B A , Cone R D . Endocrinology , 1996 , 137 ( 5 ): 2043 - 2050 . Endocrinology Thomas M , Keramidas M , Monchaux E , et al . Microsc Res Techniq , 2003 , 61 ( 3 ): 247 - 251 . Microsc Res Techniq Sewer M B , Waterman M R , Microsc Res Techniq , 2003 , 61 ( 3 ): 300 - 307 . Microsc Res Techniq Dallman M F , la-Fleur S E , Pecoraro N C , et al . Endocrinology , 2004 , 145 ( 6 ): 2633 - 2638 . Endocrinology Vaidyanathan G , Zalutsky M R . Nucl Med Biol , 1992 , 19 ( 3 ): 275 - 281 . Nucl Med Biol Vaidyanathan G , Zalutsky M R . Bioconjugate Chem , 1994 , 5 ( 4 ): 352 - 356 . Bioconjugate Chem Mading P , Fuchtner F , Wust F . Appl Radiat Isot , 2005 , 63 ( 3 ): 329 - 332 . Appl Radiat Isot Wust F , Hultsch C , Bergmann R , et al . Appl Radiat Isot , 2003 , 59 ( 1 ): 43 - 48 . Appl Radiat Isot Cheng D , Yin D , Zhang L , et al . J Fluorine Chem , 2007 , 128 ( 3 ): 196 - 201 . J Fluorine Chem Jalilian A R , Shanehsazzadeh S , Akhlaghi M , et al . J Radioanal Nucl Ch , 2003 , 278 ( 1 ): 123 - 129 . J Radioanal Nucl Ch Jalilian A R , Shanehsazzadeh S , Akhlaghi M , et al . Radiochim Acta , 2008 , 96 : 435 - 439 . Radiochim Acta Toretsky J , Levenson A , Weinberg I N , et al . Nucl Med Biol , 2004 , 31 ( 6 ): 747 - 752 . Nucl Med Biol Haka M S , Kilboum M R , Watkins G L , et al . J Labelled Cmpd Radiopharm , 1989 , 27 ( 7 ): 823 - 833 . J Labelled Cmpd Radiopharm SYNACTHEN DEPOT.® Data Sheet, Novartis New Zealand Limited Private Bag 47909 Ponsonby 6-8 Mackelvie Street, Grey Lynn AUCKLAND , 15 Feb., 2006 SYNACTHEN DEPOT.® Data Sheet, Novartis New Zealand Limited Private Bag 47909 Ponsonby 6-8 Mackelvie Street, Grey Lynn AUCKLAND Harmer S C , Pepper D J , Cooke K , et al . J Endocrinol , 2008 , 196 ( 1 ): 149 - 158 . J Endocrinol Noon L A , Bakmanidis A , Clark A J L , et al . J Mol Endocrinol , 2006 , 37 ( 3 ): 415 - 420 . J Mol Endocrinol O’shaughnessy P J , Fleming L M , Jackson G , et al . Endocrinology , 2003 , 144 ( 8 ): 3279 - 3284 . Endocrinology 10.13538/j.1001-8042/nst.20.163-169 2009-03-06 2009-06-20 2021-01-19 2009 Nuclear Science and Techniques 03 20

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

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