Skip to main content
SpringerLink
Log in

Synthesis, quality control and tissue distribution of 2-[18F]-nicotinic acid diethylamide, a potential agent for regional cerebral function studies

  • Medical Radionuclides and the Quality of Radiopharmaceuticals
  • Published:
Journal of Radioanalytical Chemistry Aims and scope Submit manuscript

Abstract

2-[18F]-nicotinic acid diethylamide was prepared by nucleophilic aromatic substitution in an acetamide melt of the corresponding chloro-compound and purified by high pressure liquid chromatography. Optimization of the reaction conditions led to a maximum radiochemical yield of about 50% within less than one half-life of18F. Tissue distribution of 2-[18F]-nicotinic acid diethylamide in various organs of mice showed a very fast accumulation of activity in the brain (mean body concentration MBC-239%) with a brain to blood ratio of 1.34.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

References

  1. For a review, see W. A. SHEPPARD, C. M. SHARTS, Organic Fluorine Chemistry, W. A. Benjamin, Inc., New York (1969), R. D. CHAMBERS, Fluorine in Organic Chemistry, J. Wiley and Sons, New York, 1973.

    Google Scholar 

  2. F. CACACE, A. P. WOLF, J. Am. Chem. Soc., 100 (1978) 3639.

    Article  CAS  Google Scholar 

  3. F. S. ROWLAND, J. A. CRAMER, R. S. IYER, R. MILSTEIN, R. L. WILLIAMS, Radiopharmaceuticals and Labelled Compounds. Vol. 1. Proc. Symp. New Devel. Radiopharm. Lab. Comp., Copenhagen, IAEA, Vienna (1973) p. 383.

    Google Scholar 

  4. J. A. CRAMER, F. S. ROWLAND, J. Am. Chem. Soc., 96 (1974) 6579.

    Article  CAS  Google Scholar 

  5. G. BALZ, G. SCHIEMANN, Ber. Deutsch. Chem. Ges., 60 (1927) 1186.

    Google Scholar 

  6. For a review, see E. FORCHE, Methoden der organischen Chemie, Vol. V/3 (Houben-Weyl), E. MÜLLER (Ed.), G. Thieme Verlag, Stuttgart (1962) p. 213.

    Google Scholar 

  7. R. W. GOULDING, A. J. PALMER, Intern. J. Appl. Radiat. Isotopes, 23 (1972) 133.

    Article  CAS  Google Scholar 

  8. R. M. HOYTE, S. S. LIN, D. R. CHRISTMAN, H. L. ATKINS, W. HAUSER, A. P. WOLF, J. Nucl. Med., 12 (1971) 280.

    CAS  Google Scholar 

  9. C. S. KOOK, M. F. REED, G. A. DIGENIS, J. Med. Chem., 18 (1975) 533.

    Article  CAS  Google Scholar 

  10. J. C. CLARK, R. W. GOULDING, M. ROMAN, A. J. PALMER, J. Radiochem. Radioanal. Lett., 14 (1973) 101.

    CAS  Google Scholar 

  11. T. NOZAKI, Y. TANAKA, Intern. J. Appl. Radiat. Isotopes, 18 (1967) 111.

    Article  CAS  Google Scholar 

  12. H. L. ATKINS, D. R. CHRISTMAN, J. S. FOWLER, W. HAUSER, R. M. HOYTE, J. F. KLOPPER, S. S. LIN, A. P. WOLF, J. Nucl. Med., 13 (1972) 713.

    CAS  Google Scholar 

  13. G. FIRNAU, C. NAHMIAS, S. GARNETT, J. Med. Chem., 16 (1973) 416.

    Article  CAS  Google Scholar 

  14. T. J. TEWSON, M. J. WELCH, J. Chem. Soc. Chem. Comm. (1979) 1149.

  15. T. J. TEWSON, M. MAEDA, M. J. WELCH, 3rd Intern. Symp. Radiopharm. Chem., June 16–20, 1980, Washington University, St. Louis, Missouri, USA (abstract).

  16. H. ELIAS, H. F. LOTTERHOS, Chem. Ber., 109 (1976) 1580.

    CAS  Google Scholar 

  17. H. SIMON, Praxis, 58 (1969) 1130.

    CAS  Google Scholar 

  18. W. J. R. TAYLOR, C. R. WOOLF, Intern. J. Clin. Pharm., 2 (1967) 92.

    Google Scholar 

  19. J. PORTIG, W. KORANSKY, D. WAHNER-ROEDLER, Naunyn—Schmiedeberg's Arch. Pharmacol., 274 (1972) 154.

    Article  CAS  Google Scholar 

  20. W. J. R. TAYLOR, Intern. J. Clin. Pharmacol., 2 (1969) 38.

    CAS  Google Scholar 

  21. J. H. LEWIS, J. Chromatog., 172 (1979) 295.

    Article  CAS  Google Scholar 

  22. F. UHLMANN, Zeitschr. Ges. Exp. Med., 43 (1924) 556.

    CAS  Google Scholar 

  23. E. J. KNUST, M. SCHÜLLER, G. STÖCKLIN, J. Lab. Comp. Radiopharm., 17 (1980) 353.

    Article  CAS  Google Scholar 

Download references

Author information

Author notes

  1. E. J. Knust

    Present address: Institut für Medizinische Strahlenphysik und Strahlenbiologie, Uniersitaetsklinikum Essen, Hufelandstr. 55, D 4300, Essen 1, FRG

Authors and Affiliations

  1. Institut für Chemie 1 (Nuklearchemie) der Kernforschungsanlage Jülich GmbH, D-517, Jülich, (FRG)

    E. J. Knust, C. Müller-Platz & M. Schüller

Authors
  1. E. J. Knust
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. C. Müller-Platz
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. M. Schüller
    View author publications

    You can also search for this author in PubMed Google Scholar

Rights and permissions

Reprints and permissions

About this article

Cite this article

Knust, E.J., Müller-Platz, C. & Schüller, M. Synthesis, quality control and tissue distribution of 2-[18F]-nicotinic acid diethylamide, a potential agent for regional cerebral function studies. J. Radioanal. Chem. 74, 283–291 (1982). https://doi.org/10.1007/BF02520379

Download citation

  • Received:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF02520379

Keywords

Search

Navigation