CAJ | 학술논문

具有生物活性的多肽类药物是目前医用放射性诊疗药物研发的一个热点，开辟了核医学分子影像剂的一个新领域。受体特异性的活性肽具有较好的药代动力学特性，且容易进行结构修饰和放射性标记，受到受体显像和肿瘤靶向性定位领域研究人员的广泛关注。一些多肽类放射性药物已经用于临床及临床前试验，且大量的多肽正有待开发。多肽的放射性标记技术经过多年的发展，已经建立起了系统的方法。通过这些方法获得的放射性药物不会影响多肽的生理活性。本文选用了两种18F标记多肽的方法，通过标记条件、放化产率、标记物的比活度、放化纯度、稳定性及荷瘤鼠体内分布等方面对两种标记方法进行比较研究，为18F标多肽类放射性药物的研究提供借鉴。
구유생물활성적다태류약물시목전의용방사성진료약물연발적일개열점，개벽료핵의학분자영상제적일개신영역。수체특이성적활성태구유교호적약대동역학특성，차용역진행결구수식화방사성표기，수도수체현상화종류파향성정위영역연구인원적엄범관주。일사다태류방사성약물이경용우림상급림상전시험，차대량적다태정유대개발。다태적방사성표기기술경과다년적발전，이경건립기료계통적방법。통과저사방법획득적방사성약물불회영향다태적생리활성。본문선용료량충18F표기다태적방법，통과표기조건、방화산솔、표기물적비활도、방화순도、은정성급하류서체내분포등방면대량충표기방법진행비교연구，위18F표다태류방사성약물적연구제공차감。
Background: Some radiopharmaceuticals based on peptides have been applied in preclinical and clinical trials, in the meantime, a large number of peptides are to be exploited. After years of development, radiolabeling techniques of peptides have progressed to be a system method. Through these methods of radiolabeling, peptides’ physiological activities would be influenced.Purpose:In this paper, we summarized two current commonly used18F labeling methods for preparation of radiopharmaceuticals based on peptides.Methods: By comparison of labeling conditions, radiochemistry yields, specific activity of labeling products, radiochemistry purity, stability and pharmacokinetics of final products, we evaluated advantages and disadvantages of the two methods, with the hope to provide reference data for future research of18F-labeled peptide radiopharmaceuticals.Results:Both [18F]SFB and Al18F-NOTA could readily label RGDyk peptide with18F, with a radiochemistry yield of about 8.5% and 15%, respectively. [18F]SFB could produce radiolabeled peptides with better specific activity, while Al18F-NOTA proved to be a more time-saving method. For stability test, more than 80% of both [18F]SFB and Al18F-NOTA could maintain intact in PBS (Phosphate Buffer Solution) or BSA (Bovine Serum Albumin) within 360 min, and about 50% radiolabeled peptides could survivein vivo.Conclusion: Thein vitroand in vivo stability of [18F]-RGD obtained with both methods were excellent, and biodistribution pattern of radiolabeled productsvia two methods did not show obvious differences.