用短寿命正电子发射体氟-18对多聚神经降压素（8-13）类似物进行放射性标记。
Radiolabeling of multimeric neurotensin(8-13) analogs with the short-lived positron emitter fluorine-18.
作者信息
Hultsch Christina, Berndt Mathias, Bergmann Ralf, Wuest Frank
机构信息
Institute of Radiopharmacy, Research Center Rossendorf, P.O. Box 51 01 19, D-01314 Dresden, Germany.
出版信息
Appl Radiat Isot. 2007 Jul;65(7):818-26. doi: 10.1016/j.apradiso.2007.02.004. Epub 2007 Mar 6.
Three methods for (18)F-labeling of dimeric and tetrameric neurotensin(8-13) derivatives were evaluated with respect to the labeling yield and the required peptide amounts. Labeling using N-succinimidyl-4-[(18)F]fluorobenzoate ([(18)F]SFB) gave low radiochemical yield for the dimeric peptides. Coupling of the tetramer with [(18)F]SFB was not successful. High yields were obtained for labeling of the aminooxy-functionalized neurotensin(8-13) dimer using 4-[(18)F]fluorobenzaldehyde ([(18)F]FBA) whilst coupling of the corresponding tetramer gave only low yields. Labeling of sulfydryl-functionalized neurotensin(8-13) derivatives using the maleinimide 4-[(18)F]fluorobenzaldehyde-O-[6-(2,5-dioxo-2,5-dihydro-pyrrol-1-yl)-hexyl]-oxime ([(18)F]FBAM) resulted in high radiochemical yields for both, the dimer and the tetramer. Therefore, [(18)F]FBAM seems to be the most suitable (18)F-labeling agent for multivalent neurotensin(8-13) derivatives.
针对标记产率和所需肽量，评估了三种用于二聚体和四聚体神经降压素(8 - 13)衍生物的(18)F标记方法。使用N-琥珀酰亚胺基-4-[(18)F]氟苯甲酸酯([(18)F]SFB)进行标记时，二聚体肽的放射化学产率较低。四聚体与[(18)F]SFB的偶联未成功。使用4-[(18)F]氟苯甲醛([(18)F]FBA)对氨氧基官能化的神经降压素(8 - 13)二聚体进行标记可获得高产率，而相应四聚体的偶联产率仅较低。使用马来酰亚胺4-[(18)F]氟苯甲醛-O-[6-(2,5-二氧代-2,5-二氢吡咯-1-基)己基]肟([(18)F]FBAM)对巯基官能化的神经降压素(8 - 13)衍生物进行标记，二聚体和四聚体均获得了高放射化学产率。因此，[(18)F]FBAM似乎是用于多价神经降压素(8 - 13)衍生物的最合适的(18)F标记剂。
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