en Medical Physics Medical Physics تحقيق بديع Original Research <div style="text-align: justify;">Background: Based on the principle of oxime formation, ¹⁸F labeling of polypeptides can be achieved via a reaction between an aldehyde group-containing ¹⁸F-prosthetic group and an aminooxy-modified polypeptide. The focus of this study was to investigate the one-step synthesis of 2-[¹⁸F] fluoro-2-deoxyglucose (¹⁸F-FDG)- arginine-arginine-leucine (RRL) from open-ring ¹⁸F-FDG and the aminooxy-modified RRL peptide cyclo(RRLfK)-ONH₂ and to study the biological distribution of ¹⁸F-FDG-RRL in a nude mouse model of human neuroglioma. Materials and Methods: The aminooxy-modified RRL peptide cyclo(RRLfK)-ONH₂ was used as the precursor to react with ¹⁸F-FDG at 100 ℃ and different pH values for 30 minutes to synthesize ¹⁸F-FDG-RRL. The labeling yield, radiochemical purity, and in-vitro stability of the product were measured, and the biological distribution of ¹⁸F-FDG-RRL in tumor-bearing nude mice was analyzed at 30 minutes, 60 minutes and 120 minutes. Results: The labeling yield of ¹⁸F-FDG-RRL was (25.5&plusmn;5.0) % at a pH of 2.0, and its radiochemical purity was greater than 95%. ¹⁸F-FDG-RRL was mainly excreted through the kidneys, with rapid blood clearance. One hour after injection, the uptake of ¹⁸F-FDG-RRL in tumors was (1.83&plusmn;0.12) injected dose per gram of tissue (%ID/g), with a tumor/muscle ratio of 7.03&plusmn;0.04, a tumor/blood ratio of 4.36&plusmn;0.21 and a tumor/brain ratio of 7.53&plusmn;1.37. Conclusion: The synthesis of ¹⁸F-FDG-RRL can be achieved through oximation. This method is straightforward and easy to promote. ¹⁸F-FDG-RRL has rapid blood clearance and high uptake by tumors.</div> Oxime, 2-fluoro-2-deoxyglucose, arginine-arginine-leucine, peptide. 357 363 http://ijrr.com/browse.php?a_code=A-10-2188-5&slc_lang=en&sid=1 R.F. Wang 7900319475328460020107 7900319475328460020107 No Department of Nuclear Medicine, Peking University First Hospital, Beijing, China Z.G. Wang 7900319475328460020108 7900319475328460020108 No Department of Nuclear Medicine, the Affiliated Hospital of Qingdao University, Qingdao, China M.M. Yu mingmingyu@vip.sina.com 7900319475328460020109 7900319475328460020109 Yes Department of Nuclear Medicine, the Affiliated Hospital of Qingdao University, Qingdao, China Y.H. Chen 7900319475328460020110 7900319475328460020110 No Intensive Care Unit, the Affiliated Hospital of Qingdao University, Qingdao, China B. Shi 7900319475328460020111 7900319475328460020111 No Department of Nuclear Medicine, the Affiliated Hospital of Qingdao University, Qingdao, China W. Xue 7900319475328460020112 7900319475328460020112 No Department of Nuclear Medicine, the Affiliated Hospital of Qingdao University, Qingdao, China