Journal of Labelled Compounds and Radiopharmaceuticals

Cover image for Vol. 55 Issue 2

February 2012

Volume 55, Issue 2

Pages i–iv, 57–95

  1. Cover and Masthead

    1. Top of page
    2. Cover and Masthead
    3. Research Articles
    1. Editorial Board (pages i–iv)

      Version of Record online: 15 FEB 2012 | DOI: 10.1002/jlcr.2909

  2. Research Articles

    1. Top of page
    2. Cover and Masthead
    3. Research Articles
    1. A fast, simple, and reproducible automated synthesis of [18F]FPyKYNE-c(RGDyK) for αvβ3 receptor positron emission tomography imaging (pages 57–60)

      Ana C. Valdivia, Miriam Estrada, Tayebeh Hadizad, Duncan J. Stewart, Rob S. Beanlands and Jean N. DaSilva

      Version of Record online: 16 NOV 2011 | DOI: 10.1002/jlcr.1948

      Thumbnail image of graphical abstract

      A new 18F labeled RGD peptide, [18F]-FPyKYNE-c(RGDyK) was synthesized via ‘click chemistry’ using [18F]FPyKYNE as prosthetic group in high purity and yield. All the steps, including a simple and convenient purification of the prosthetic group were carried out in a fully automated process.

    2. Synthesis of [D4]- and [D7]-4β-hydroxycholesterols for use in a novel drug–drug interaction assay (pages 61–65)

      Wesley A. Turley, Richard C. Burrell, Samuel J. Bonacorsi Jr, Angela K. Goodenough and Joelle M. Onorato

      Version of Record online: 8 DEC 2011 | DOI: 10.1002/jlcr.1952

      Thumbnail image of graphical abstract

      Recent studies have shown 4β–hydroxycholesterol as an endogenous biomaker of CYP3A activity and predictor of potential drug–drug interactions. This article describes the synthesis of stable isotope labeled 4β–hydroxycholesterol [D4]-1 and [D7]-1. The labeled compounds were needed to assist in the development of a drug–drug interaction assay to measure 4β–hydroxycholesterol in clinical plasma samples following treatment with a CYP3A inducer or inhibitor.

    3. Site-specific 2H-labeled oleic acid and derived esters for use as tracers of ethyl oleate metabolism in honey bees (pages 66–70)

      Hao Chen and Erika Plettner

      Version of Record online: 8 DEC 2011 | DOI: 10.1002/jlcr.1953

      Thumbnail image of graphical abstract

      A synthetic route for the efficient preparation of a site-specific deuterium labeled oleic acid (11) from readily available starting materials such as 1 and 5 has been developed. Several derived esters were also prepared. The labeled precursors have been used as powerful probes in the study of biosynthesis of a primer pheromone ethyl oleate in honeybees.

    4. A novel bifunctional chelating agent based on bis(hydroxamamide) for 99mTc labeling of polypeptides (pages 71–79)

      Masahiro Ono, Masatsugu Ohgami, Mamoru Haratake, Hideo Saji and Morio Nakayama

      Version of Record online: 12 DEC 2011 | DOI: 10.1002/jlcr.1954

      Thumbnail image of graphical abstract

      We successfully designed and synthesized C3(BHam)2―COOH as a new bifunctional chelating agent for 99mTc labeling of polypeptides. C3(BHam)2―COOH formed a stable 99mTc complex and enabled us to prepare 99mTc-labeled polypeptides by using a TFP active ester of C3(BHam)2―COOH. 99mTc-C3(BHam)2―polypeptides provided radiometabolites, which showed rapid elimination from the liver.

    5. Tritium labeling of a γ-secretase inhibitor and two modulators as in vitro imaging agents (pages 80–83)

      Jonas Malmquist, Alexandra Bernlind, Johan Sandell, Peter Ström and Magnus Waldman

      Version of Record online: 23 JAN 2012 | DOI: 10.1002/jlcr.1955

      Thumbnail image of graphical abstract

      [3H]DBZ, [3H]1, and [2-3H]AZ8349 are promising in vitro imaging radioligands and have the potential to provide key information with regard to γ-secretase expression, function, stoichiometry, and pharmacology.

    6. Proton exchange reactions in isotope chemistry (I) (pages 84–87)

      Zhigang Jian, Tapan Ray, Amy Wu and Lawrence Jones

      Version of Record online: 23 JAN 2012 | DOI: 10.1002/jlcr.1959

      Thumbnail image of graphical abstract

      Direct H-D exchange reactions were applied to the preparations of stable isotope labeled TKI258 and two TKI258 metabolites. Each compound was made in one single H-D exchange reaction in the presence of deuterium phosphoric acid-BF3 complex with excellent isotope incorporation. The number of deuterium incorporation and deuterium distribution in the molecules was discussed.

    7. Syntheses of deuterium-labelled cholesteryl neoglycolipids (pages 88–95)

      Dominique Lafont, Paul Boullanger and Antoine Gambetta

      Version of Record online: 25 JAN 2012 | DOI: 10.1002/jlcr.1961

      Thumbnail image of graphical abstract

      The synthesis of four deuterium-labelled cholesteryl triethyleneglycol neoglycolipids of N-acetyl-D-glucosamine is described. Deuterium atoms were incorporated either as a CD2 group in the triethyleneglycol spacer or as a trideuteroacetamido function on the carbohydrate head.