Pike V W, Palmer A J, Horlock P L, Perun T J, Freiberg L A, Dunnigan D A, Liss R H
Int J Appl Radiat Isot. 1984 Feb;35(2):103-9. doi: 10.1016/0020-708x(84)90192-3.
A fast semi-automated method is described for labeling the antibiotic, erythromycin A (1), with the short-lived positron-emitting radionuclide, 11C (t 1/2 = 20.4 min), in order to permit the non-invasive study of its tissue uptake in vivo. Labelling was achieved by the fast reductive methylation of N-demethylerythromycin A (2) with [11C]formaldehyde, itself prepared from cyclotron-produced [11C]-carbon dioxide. Rapid chemical and radiochemical purification of the [N-methyl-11C]erythromycin A (3) were achieved by HPLC and verified by TLC with autoradiography. The purified material was formulated for human i.v. injection as a sterile apyrogenic solution of the lactobionate salt. The preparation takes 42 min from the end of radionuclide production and from [11C]carbon dioxide produces [N-methyl-C11]erythromycin A lactobionate in 1-12% radiochemical yield, corrected for radioactive decay.
本文描述了一种快速半自动方法，用于用短寿命正电子发射放射性核素(^{11}C)（半衰期(t_{1/2}=20.4)分钟）标记抗生素红霉素A（1），以便在体内对其组织摄取进行非侵入性研究。标记是通过用[ (^{11}C) ]甲醛对N - 去甲基红霉素A（2）进行快速还原甲基化来实现的，[ (^{11}C) ]甲醛本身由回旋加速器产生的[ (^{11}C) ]二氧化碳制备。通过高效液相色谱法（HPLC）对[ (N) - 甲基 - (^{11}C) ]红霉素A（3）进行快速化学和放射化学纯化，并通过放射自显影薄层色谱法（TLC）进行验证。纯化后的物质配制成用于人体静脉注射的乳糖酸盐无菌无热原溶液。从放射性核素生产结束起，该制备过程耗时42分钟，以[ (^{11}C) ]二氧化碳为原料，经放射性衰变校正后，[ (N) - 甲基 - (^{11}C) ]红霉素A乳糖酸盐的放射化学产率为1 - 12%。
