【摘要】 目的研究 O-(2-¹⁸F-氟代乙基)-L-酪氨酸(¹⁸F-FET)新的一步直接亲核放射氟化法合成路线及其生物学评价。方法以 N-叔丁氧羰基-（O-（2-对甲苯磺酰乙氧基））-L-酪氨酸甲酯[N-BOC-（O-TsE）-L-Tyr-OMe]为标记前体,采用直接亲核放射氟化法合成 ¹⁸F-FET,并用体内外稳定性和药代动力学实验评价其生物学性能。结果 ¹⁸F-FET 的合成时间约为50 min,放化产率为40%（未经衰减校正）,放化纯>97%。体内外稳定性好,在 PBS 中放置3个半衰期后,放化纯没有变化;注射 ¹⁸F-FET后1 h 内小鼠血样示踪没有发现代谢产物。¹⁸F-FET 在动物体内的时间-血药浓度曲线符合二室模型,分布相较短,消除相很长,适合显像。结论用该合成路线标记前体易得,合成时间短,放化产率高,产物具有良好的体内行为。更多还原

【Abstract】 Objective To investigate a novel synthetic method and biological evaluation of O-(2-¹⁸F- fluoroethyl)-L-tyrosine(¹⁸F-FET)as metabolic PET tracer for brain tumor imaging.Methods ¹⁸F-FET was synthesized via one-step direct nueleophilic radiofluorination from a easily obtained precursor N-butyloxycar- bonyl-（O-（2-tosyloxyethyl））-L-tyrosine methyl ester.Its biological evaluation was performed by experi- ments with in vivo and in vitro stability tests and its pharmacokineties.Results ¹⁸F-FET was prepared within 50 min with good radiochemical yield（40%,decay not corrected）and radiochemical purity（> 97%）.The radiochemical purity was not changed after incubation with PBS for 3 half-life of ¹⁸F and no me- taboliles were found within 1 h,and it also demonstrated that this tracer was very stable in vivo and in vitro. The pharmacokinetics was fitted to two-compartment model with short distribution phase and long clearance phase.Conclusions ¹⁸F-FET was prepared via direct nucleophilic radiofluorination starting from an easily obtained precursor with shortened synthetic time and good radiochemical yield.It was possessed of good bio- logical properties for brain tumor PET imaging.更多还原