Journal of Labelled Compounds and Radiopharmaceuticals

Cover image for Vol. 55 Issue 7

15 June 2012

Volume 55, Issue 7

Pages i–iv, 235–280

  1. Cover and Masthead

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

      Article first published online: 25 JUN 2012 | DOI: 10.1002/jlcr.2943

  2. Reviews Articles

    1. Top of page
    2. Cover and Masthead
    3. Reviews Articles
    4. Research Articles
    1. Tritium: a coming of age for drug discovery and development ADME studies (pages 235–257)

      W. J. S. Lockley, A. McEwen and R. Cooke

      Article first published online: 19 JUN 2012 | DOI: 10.1002/jlcr.2928

      Thumbnail image of graphical abstract

      Recent developments in tritium chemistry and analysis mean that high-quality tritium-labelled drugs can now be prepared simply, cheaply and in timescales commensurate with those needed for rapid drug discovery projects. This rapid-labelling approach is ensuring more effective pharmaceutical research projects, a key issue in commercial success. At later stages in the pharmaceutical development process, the same tritium labelling and analysis methodologies can also be utilised to support high quality adsorption, distribution, metabolism and excretion studies.

  3. Research Articles

    1. Top of page
    2. Cover and Masthead
    3. Reviews Articles
    4. Research Articles
    1. Synthesis of S-thiomethyl DMSA and S-thiomethyl ECD, radiolabelling with technetium-99m and biological evaluation (pages 258–263)

      Kasturi Sanyal and Mita Chatterjee Debnath

      Article first published online: 14 JUN 2012 | DOI: 10.1002/jlcr.2922

      Thumbnail image of graphical abstract

      Synthesis of S-thiomethyl dimercaptosuccinic acid (DMSA) and S-thiomethyl ethylenedi-L-cysteine diethyl ester (ECD) was carried out where protection of the free thiolate group increased the stability of the ligand and automatic deprotection resulted in the desired radiopharmaceutical. The results suggest that the protection by S-thiomethylation could be utilized for the development of single-vial DMSA and ECD kit.

    2. Radiosynthesis and biological evaluation of the M1 muscarinic acetylcholine receptor agonist ligand [11C]AF150(S) (pages 264–273)

      Hans J.C. Buiter, Josée E. Leysen, Robert C. Schuit, Abraham Fisher, Adriaan A. Lammertsma and Albert D. Windhorst

      Article first published online: 11 MAY 2012 | DOI: 10.1002/jlcr.2932

      Thumbnail image of graphical abstract

      [11C]AF150(S) was successfully synthesized, yielding 69 ± 9%, with radiochemical purity >99%. The measured logDoct,7.4 was 0.05. Autoradiography showed binding in M1 muscarinic acetylcholine receptor (M1ACh-R)-rich brain areas and selective inhibition by muscarinic agents in conditions promoting agonist binding. Biodistribution studies revealed high brain uptake, to levels exceeding five times that in blood. In addition, rapid metabolism was observed. In M1ACh-R-rich areas, specific uptake versus cerebellum was observed. It provides an interesting lead for the development of an M1ACh-R-agonist positron emission tomography ligand meant to explore the active receptor state.

    3. Preparation and preliminary bioevaluation of a 99mTc(CO)3-glucose derivative prepared by a click chemistry route (pages 274–280)

      Soledad Fernández, Nancy Crócamo, Marcelo Incerti, Javier Giglio, Laura Scarone and Ana Rey

      Article first published online: 24 MAY 2012 | DOI: 10.1002/jlcr.2933

      Thumbnail image of graphical abstract

      Preliminary bioevaluation of a new 99mTc(CO)3-glucose derivative complex is presented. Derivatization of glucose at C2 was achieved using the so-called ‘click chemistry’ route, forming a histidine-like, 1,4-disubstituted triazole adequate as donor atom system for Tc(I)-tricarbonyl complexes. Compared with [18F]-2-fluoro-2-deoxy-d-glucose (FDG), biodistribution in the same animal model was very similar, although tumour uptake was significantly higher for [18F]-FDG probably because of high hidrophilicity that may hinder cell penetration. Further modifications of the chelator and linker to increase lipophilicity might improve biological results.

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