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Radiolabeling of multimeric neurotensin(8-13) analogs with the short-lived positron emitter fluorine-18

Abstract

Three methods for {sup 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-[{sup 18}F]fluorobenzoate ([{sup 18}F]SFB) gave low radiochemical yield for the dimeric peptides. Coupling of the tetramer with [{sup 18}F]SFB was not successful. High yields were obtained for labeling of the aminooxy-functionalized neurotensin(8-13) dimer using 4-[{sup 18}F]fluorobenzaldehyde ([{sup 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-[{sup 18}F]fluorobenzaldehyde-O-[6-(2,5-dioxo-2,5-dihydro-pyrrol-1-yl)-hexyl] -oxime ([{sup 18}F]FBAM) resulted in high radiochemical yields for both, the dimer and the tetramer. Therefore, [{sup 18}F]FBAM seems to be the most suitable {sup 18}F-labeling agent for multivalent neurotensin(8-13) derivatives.
Authors:
Hultsch, Christina; [1]  Berndt, Mathias; [1]  Bergmann, Ralf; [1]  Wuest, Frank [1] 
  1. Institute of Radiopharmacy, Research Center Rossendorf, P.O. Box 51 01 19, D-01314 Dresden (Germany)
Publication Date:
Jul 15, 2007
Product Type:
Journal Article
Resource Relation:
Journal Name: Applied Radiation and Isotopes; Journal Volume: 65; Journal Issue: 7; Other Information: DOI: 10.1016/j.apradiso.2007.02.004; PII: S0969-8043(07)00071-1; Copyright (c) 2007 Elsevier Science B.V., Amsterdam, The Netherlands, All rights reserved; Country of input: International Atomic Energy Agency (IAEA)
Subject:
07 ISOTOPES AND RADIATION SOURCES; FLUORINE 18; LABELLING; NEOPLASMS; PEPTIDES; POSITRONS; RADIOCHEMISTRY; RADIOPHARMACEUTICALS
OSTI ID:
20978791
Country of Origin:
United Kingdom
Language:
English
Other Identifying Numbers:
Journal ID: ISSN 0969-8043; ARISEF; TRN: GB07R4126007500
Submitting Site:
GBN
Size:
page(s) 818-826
Announcement Date:
Mar 10, 2008

Citation Formats

Hultsch, Christina, Berndt, Mathias, Bergmann, Ralf, and Wuest, Frank. Radiolabeling of multimeric neurotensin(8-13) analogs with the short-lived positron emitter fluorine-18. United Kingdom: N. p., 2007. Web. doi:10.1016/j.apradiso.2007.02.004.
Hultsch, Christina, Berndt, Mathias, Bergmann, Ralf, & Wuest, Frank. Radiolabeling of multimeric neurotensin(8-13) analogs with the short-lived positron emitter fluorine-18. United Kingdom. doi:10.1016/j.apradiso.2007.02.004.
Hultsch, Christina, Berndt, Mathias, Bergmann, Ralf, and Wuest, Frank. 2007. "Radiolabeling of multimeric neurotensin(8-13) analogs with the short-lived positron emitter fluorine-18." United Kingdom. doi:10.1016/j.apradiso.2007.02.004. https://www.osti.gov/servlets/purl/10.1016/j.apradiso.2007.02.004.
@misc{etde_20978791,
title = {Radiolabeling of multimeric neurotensin(8-13) analogs with the short-lived positron emitter fluorine-18}
author = {Hultsch, Christina, Berndt, Mathias, Bergmann, Ralf, and Wuest, Frank}
abstractNote = {Three methods for {sup 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-[{sup 18}F]fluorobenzoate ([{sup 18}F]SFB) gave low radiochemical yield for the dimeric peptides. Coupling of the tetramer with [{sup 18}F]SFB was not successful. High yields were obtained for labeling of the aminooxy-functionalized neurotensin(8-13) dimer using 4-[{sup 18}F]fluorobenzaldehyde ([{sup 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-[{sup 18}F]fluorobenzaldehyde-O-[6-(2,5-dioxo-2,5-dihydro-pyrrol-1-yl)-hexyl] -oxime ([{sup 18}F]FBAM) resulted in high radiochemical yields for both, the dimer and the tetramer. Therefore, [{sup 18}F]FBAM seems to be the most suitable {sup 18}F-labeling agent for multivalent neurotensin(8-13) derivatives.}
doi = {10.1016/j.apradiso.2007.02.004}
journal = {Applied Radiation and Isotopes}
issue = {7}
volume = {65}
place = {United Kingdom}
year = {2007}
month = {Jul}
}