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Title: Simple and fast {sup 18}F-labeling of proteins by coupling with photogenerated [{sup 18}F] arylnitrene

Journal Article · · Journal of Nuclear Medicine
OSTI ID:197940
; ;  [1]
  1. Stoecklin Institut fuer Nuklearchemie, Juelich (Germany); and others

Radiolabeled antibodies are of increasing interest for diagnosis and radiotherapy of various diseases. For a potential routine application of {sup 18}F-labeled antibodies and other proteins with PET we have developed a fast two step n.c.a. radiofluorination method in analogy to a recent radiodination procedure. After introduction of [{sup 18}F]-fluoride into commercially available 4-azidophenacyl-bromide (APB) by nucleophilic substitution and subsequent purification by HPLC and Sep Pak C-18 filtration, the n.c.a. 4-azidophenacyl-[{sup 18}F]fluoride ([{sup 18}F]APF) was obtained with a radiochemical yield of 71{plus_minus}5% within about 30 min. Labeling of proteins in aqueous solution was achieved by reaction of the [{sup 18}F]nitrene formed by UV irradiation of the [{sup 18}F]APF at 366 nm in the presence of the substrate. The photoreaction is completed within 6-8 min. Final purification of the labeled protein was performed by size exclusion chromatography. Using this method, human serum albumine, transferrin, avidin and IgG was labeled in RCY up to 25% within 45 min.

OSTI ID:
197940
Report Number(s):
CONF-940605-; ISSN 0161-5505; TRN: 95:007029-0080
Journal Information:
Journal of Nuclear Medicine, Vol. 35, Issue Suppl.5; Conference: 41. annual meeting of the Society of Nuclear Medicine, Orlando, FL (United States), 5-8 Jun 1994; Other Information: PBD: May 1994
Country of Publication:
United States
Language:
English