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Journal of Nuclear Medicine

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Meeting ReportMolecular Targeting Probes Track

Automated radiosynthesis of 18F-FBEM, a sulfhydryl site specific labeling agent for peptides and proteins

Keunpoong Lim, Jim Ropchan, David Labaree, Dale Kiesewetter, Xiaoyuan Chen and Yiyun Huang
Journal of Nuclear Medicine May 2016, 57 (supplement 2) 276;
Keunpoong Lim
2Yale University New Haven CT United States
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Jim Ropchan
2Yale University New Haven CT United States
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David Labaree
2Yale University New Haven CT United States
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Dale Kiesewetter
1NIH Bethesda MD United States
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Xiaoyuan Chen
1NIH Bethesda MD United States
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Yiyun Huang
2Yale University New Haven CT United States
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Abstract

276

Objectives In the process of developing 18F-FBEM-(Cys40)-exendin-4 for imaging the glucagon-like peptide 1 receptor (GLP-1R) in the pancreas, we have instituted a robust automated synthesis of 18F-FBEM, a sulfhydryl (-SH) site specific agent for radiolabeling of peptides and proteins.

Methods Radiosynthesis of 18F-FBEM was performed in a TRACERlab FXN-Pro module using a 3-step reaction sequence in two separate reactors. Each step of the automated process was optimized during a series of test runs. In reactor 1, the ammonium salt precursor 1 (2-3 mg) was reacted with dried 18F-/K222 in DMSO (0.4 mL) at 105 °C for 10 min to generate 2, which was hydrolyzed to 3 by heating with 0.1 N NaOH (0.2 mL) at 95 °C for 5 min. After neutralization with 0.2 N HCl (0.2 mL), the reaction mixture was diluted with two portions of water (5 mL each) and passed separately through a Waters C18 Light SepPak. The intermediate 3 was then eluted with 1 mL of CH3CN/DMSO (3/1, v/v) into the second reactor of the module, and a solution of N-(2-aminoethyl) maleimide (3-5 mg) in DMSO (0.2 mL) was added, followed by DECP and DIPEA in 0.1 mL of CH3CN each. The reaction mixture was heated at 70 °C for 7 min, diluted with 1mM HCl and purified by preparative HPLC. Dilution of of the HPLC fraction, solid phase extraction on a second C18 Light SepPak catridge, and elution with CH3CN (1 mL) gave pure 18F-FBEM (4).

Results The fully automated, two-pot, three-step radiosynthesis generated 1.67-3.89 GBq of of 18F-FBEM from 22.2 GBq of starting 18F-fluoride.The radiochemical yield ranged from 7.5 to 17.5% (non-decay corrected), with specific activity of 31.8±5.3 MBq/nmol (n=3) at the end of synthesis. Radiochemical purity of 18F-FBEM was greater than 98%, and total synthesis time was ~90 min.

Conclusions We have developed a robust automated method to synthesize 18F-FBEM using a FXN-Pro module. 18F-FBEM was then used in the radiolabeling of (Cys40)-exendin-4 to produce 18F-FBEM-(Cys40)-exendin-4 for imaging of GLP-1R in the pancreas of normal and diabetic rats. $$graphic_016BB236-D290-40FB-B2C9-F5FC83A07042$$

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Journal of Nuclear Medicine
Vol. 57, Issue supplement 2
May 1, 2016
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Automated radiosynthesis of 18F-FBEM, a sulfhydryl site specific labeling agent for peptides and proteins
Keunpoong Lim, Jim Ropchan, David Labaree, Dale Kiesewetter, Xiaoyuan Chen, Yiyun Huang
Journal of Nuclear Medicine May 2016, 57 (supplement 2) 276;

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Automated radiosynthesis of 18F-FBEM, a sulfhydryl site specific labeling agent for peptides and proteins
Keunpoong Lim, Jim Ropchan, David Labaree, Dale Kiesewetter, Xiaoyuan Chen, Yiyun Huang
Journal of Nuclear Medicine May 2016, 57 (supplement 2) 276;
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