Journal of Labelled Compounds and Radiopharmaceuticals

Cover image for Vol. 57 Issue 4

Special Issue: Current Developments in PET and SPECT Imaging

April 2014

Volume 57, Issue 4

Pages i–iv, 191–331

Issue edited by: Jonathan R. Dilworth, Sofia I. Pascu

  1. Issue Information

    1. Top of page
    2. Issue Information
    3. Editorial
    4. Special Issue Reviews
    5. Special Issue Articles
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    1. Issue Information (pages i–iv)

      Version of Record online: 16 APR 2014 | DOI: 10.1002/jlcr.3121

  2. Editorial

    1. Top of page
    2. Issue Information
    3. Editorial
    4. Special Issue Reviews
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    1. Recent developments in PET and SPECT imaging (pages 191–194)

      Sofia Pascu and Jon Dilworth

      Version of Record online: 16 APR 2014 | DOI: 10.1002/jlcr.3196

  3. Special Issue Reviews

    1. Top of page
    2. Issue Information
    3. Editorial
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    1. Transition metal mediated [11C]carbonylation reactions: recent advances and applications (pages 195–201)

      Steven Kealey, Antony Gee and Philip W. Miller

      Version of Record online: 14 JAN 2014 | DOI: 10.1002/jlcr.3150

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      Transition metal-mediated [11C]carbonylations are a versatile class of reaction that can be used to radiolabel a range of carbonyl functional groups in PET imaging probes. This mini review covers recent advances and applications of this class of 11CO-labelling reactions and highlights the synthesis of potential PET radiotracer molecules.

  4. Special Issue Articles

    1. Top of page
    2. Issue Information
    3. Editorial
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    1. Palladium-mediated oxidative carbonylation reactions for the synthesis of 11C-radiolabelled ureas (pages 202–208)

      Steven Kealey, Stephen M. Husbands, Idriss Bennacef, Antony D. Gee and Jan Passchier

      Version of Record online: 11 DEC 2013 | DOI: 10.1002/jlcr.3151

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      Palladium(II)-mediated oxidative carbonylation reactions have been performed for the synthesis of 11C-radiolabelled ureas via the coupling of amines with [11C]carbon monoxide. This one-pot process, beginning with the low-pressure trapping of [11C]carbon monoxide in a solution of copper(I)tris(pyrazolyl)borate, has been used to label a series of symmetrically and unsymmetrically substituted [11C]ureas in good yield.

    2. Synthesis and in vivo evaluation of 11C-labeled (1,7-dicarba-closo-dodecaboran-1-yl)-N-{[(2S)-1-ethylpyrrolidin-2-yl]methyl}amide (pages 209–214)

      Vanessa Gómez-Vallejo, Naiara Vázquez, Kiran Babu Gona, Maria Puigivila, Mikel González, Eneko San Sebastián, Abraham Martin and Jordi Llop

      Version of Record online: 5 DEC 2013 | DOI: 10.1002/jlcr.3159

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      The synthesis and in vivo evaluation of 11C-labeled (1,7-dicarba-closo-dodecaboran-1-yl)-N-{[(2S)-1-ethylpyrrolidin-2-yl]methyl}amide, an analog of the D2 receptor ligand [11C]raclopride, is described. Moderate radiochemical yields (18.2 ± 2.8%, decay corrected) were obtained in overall synthesis time of ~50 min. In vivo assays showed a biodistribution pattern with significant uptake in liver, kidneys, and lungs at short times after administration (t = 4 min) and elimination via urine. Uptake in the brain was significant but unspecific.

    3. 2-Bromo-6-[18F]fluoropyridine: two-step fluorine-18 radiolabelling via transition metal-mediated chemistry (pages 215–218)

      Helen M. Betts and Edward G. Robins

      Version of Record online: 18 DEC 2013 | DOI: 10.1002/jlcr.3147

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      The novel synthon 2-bromo-6-[18F]fluoropyridine was developed to provide a new synthetic route for molecules unsuitable for direct [18F]fluorination. 2-Bromo-6-[18F]fluoropyridine was isolated in high yield, and electron-rich [18F]fluoropyridyl compounds were subsequently prepared using palladium-mediated cross-coupling reactions. This synthon can now be widely applied in transition metal-mediated reactions.

  5. Special Issue Reviews

    1. Top of page
    2. Issue Information
    3. Editorial
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    1. For JRD/SIP special volume JLCR Al18F labeling of peptides and proteins (pages 219–223)

      Peter Laverman, William J. McBride, Robert M. Sharkey, David M. Goldenberg and Otto C. Boerman

      Version of Record online: 10 JAN 2014 | DOI: 10.1002/jlcr.3161

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      Many strategies have been developed to radiolabel peptide and proteins with fluorine-18. A straightforward approach, based on the chelation of aluminum fluoride by (1,4,7-triazacyclononane-1,4,7-triacetic acid), has been developed a few years ago. Here, we summarize the development, optimization, and applications of the Al18F labeling technology.

    2. You have full text access to this OnlineOpen article
      Chelators for copper radionuclides in positron emission tomography radiopharmaceuticals (pages 224–230)

      Zhengxin Cai and Carolyn J. Anderson

      Version of Record online: 18 DEC 2013 | DOI: 10.1002/jlcr.3165

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      The development of chelating agents for copper radionuclides in positron emission tomography radiopharmaceuticals has been a highly active and important area of study in recent years. The rapid evolution of chelators has resulted in highly specific copper chelators that can be readily conjugated to biomolecules and efficiently radiolabeled to form stable complexes in vivo. Chelators are not only designed for conjugation to monovalent biomolecules but can also be designed to be incorporated into multivalent targeting ligands such as theranostic nanoparticles. These advancements have strengthened the role of copper radionuclides in the fields of nuclear medicine and molecular imaging. This review summarizes copper chelators that have most greatly advanced the field of copper-based radiopharmaceuticals over the past 5 years.

    3. Radiocopper for the imaging of copper metabolism (pages 231–238)

      Rebekka Hueting

      Version of Record online: 14 MAR 2014 | DOI: 10.1002/jlcr.3155

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      This review discusses the contribution of copper radioisotopes for the study of copper metabolism. 64Cu and 67Cu have been used to trace the fate of copper in vitro and in vivo, both for the investigation of normal copper homeostasis and to delineate alterations found in disease. Particular focus is placed on the application of 64Cu-PET for the imaging of copper biodistribution in neurological disorders, genetic diseases and cancer.

    4. Recent advances in chelator design and labelling methodology for 68Ga radiopharmaceuticals (pages 239–243)

      Benjamin P. Burke, Gonçalo S. Clemente and Stephen J. Archibald

      Version of Record online: 4 FEB 2014 | DOI: 10.1002/jlcr.3146

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      The importance of gallium-68 in clinical radiopharmaceutical applications is increasing. This requires a reliable set of tools and methods for radiolabelling molecules to use in targeted imaging. This review details recent advances in the design of chelators for efficient and effective isotope incorporation.

    5. Nitrogen-13: historical review and future perspectives (pages 244–254)

      Vanessa Gómez-Vallejo, Vijay Gaja, Kiran B. Gona and Jordi Llop

      Version of Record online: 14 JAN 2014 | DOI: 10.1002/jlcr.3163

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      The use of 13N, a positron emitter with a half-life of 9.97 min, has been historically restricted. Paradoxically, its stable isotope is present in many biological active molecules. In this paper, the different strategies for the production of 13N in different chemical forms and their application to the preparation of 13N-labeled structures are reviewed. The current situation and future perspectives are also briefly discussed.

    6. Single amino acid chelate complexes of the M(CO)3+ core for correlating fluorescence and radioimaging studies (M = 99mTc or Re) (pages 255–261)

      Michael P. Coogan, Robert P. Doyle, John F. Valliant, John W. Babich and Jon Zubieta

      Version of Record online: 7 JAN 2014 | DOI: 10.1002/jlcr.3164

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      Complexes incorporating the Re(CO)3+ core provide robust molecular probes for fluorescent imaging. The in vitro/in vivo pairing for the Re-based fluorescent probes and the 99mTc-based radioactive imaging agents allows the assessment of the fate of the imaging agent at the cellular level in real time and the evaluation of mechanisms relevant to cellular localization and specificity. The accompanying images show the Re(CO)3+ core complexed to N,N′-bis(6,7-dihydroquinolin-2-ylmethyl)butane-1,4-diamine and its B12 conjugate [B12-bisquin-Re(CO)3]+ and cell binding and internalization of the conjugate into human placenta choriocarcinoma (BeWo) cells.

  6. Special Issue Articles

    1. Top of page
    2. Issue Information
    3. Editorial
    4. Special Issue Reviews
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    1. Rhenium and technetium tricarbonyl complexes of 1,4-Substituted pyridyl-1,2,3-triazole bidentate ‘click’ ligands conjugated to a targeting RGD peptide (pages 262–269)

      Timothy U. Connell, David J. Hayne, Uwe Ackermann, Henri J. Tochon-Danguy, Jonathan M. White and Paul S. Donnelly

      Version of Record online: 11 DEC 2013 | DOI: 10.1002/jlcr.3169

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      New 1,4-substituted pyridyl-1,2,3-triazole ligands with pendent functional groups were conjugated to a peptide containing the arginine–glycine–aspartic acid peptide motif. The synthesis and characterization rhenium and technetium carbonyl complexes, [M(CO)3Lx(py)]+ (where M = ReI or 99mTcI; Lx = 1,4-substituted pyridyl-1,2,3-triazole ligands and py = pyridine) were prepared.

  7. Special Issue Reviews

    1. Top of page
    2. Issue Information
    3. Editorial
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    1. High-valent technetium chemistry—new opportunities for radiopharmaceutical developments (pages 270–274)

      Henrik Braband

      Version of Record online: 18 DEC 2013 | DOI: 10.1002/jlcr.3148

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      fac-{99mTcO3}+ complexes are potential new synthons for radiopharmaceutical developments, due to their unique physicochemical properties and unprecedented reactivity. In this article, recent developments and the ‘state of the art’ in the field of high-valent technetium chemistry are reviewed comprehensively.

  8. Special Issue Articles

    1. Top of page
    2. Issue Information
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    1. Radiolabeled antagonistic bombesin peptidomimetics for tumor targeting (pages 275–278)

      Ibai E. Valverde, Elena Huxol and Thomas L. Mindt

      Version of Record online: 11 DEC 2013 | DOI: 10.1002/jlcr.3162

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      The replacement of amide bonds in the backbone of peptides by proteolytically stable 1,2,3-triazole isosteres can provide novel peptidomimetics with promising properties for the development of tumor-targeting radiopeptides. Application of the amide-to-triazole substitutions strategy to the antagonistic bombesin sequence JMV594 led to the identification of a 1,2,3-triazole containing radiopeptidomimetic for targeting gastrin-releasing peptide receptor over-expressing tumors.

  9. Special Issue Reviews

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    1. Prospects for enhancement of targeted radionuclide therapy of cancer using ultrasound (pages 279–284)

      Richard J. Browning, Vineeth Rajkumar, R. Barbara Pedley, Robert J. Eckersley and Philip J. Blower

      Version of Record online: 18 DEC 2013 | DOI: 10.1002/jlcr.3157

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      Ultrasound-mediated drug delivery is a promising means of enhancing delivery, distribution, and effectiveness of drugs within tumours. In this review, prospects for exploiting ultrasound to improve the tumour delivery and distribution of radiolabelled antibodies for radioimmunotherapy and to overcome barriers imposed by tumour microenvironment are discussed.

    2. The inverse electron demand Diels–Alder click reaction in radiochemistry (pages 285–290)

      Thomas Reiner and Brian M. Zeglis

      Version of Record online: 18 DEC 2013 | DOI: 10.1002/jlcr.3149

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      The inverse electron-demand Diels–Alder (IEDDA) cycloaddition between 1,2,4,5-tetrazines and strained alkene dienophiles is an emergent variety of catalyst-free click chemistry that has the potential to have a transformational impact on radiopharmaceutical science. The ligation is selective, rapid, and bioorthogonal and, since its advent in 2008, has been employed in a wide variety of chemical settings. In this review, the first applications of IEDDA click chemistry to radiochemistry are discussed, including the synthesis of 18 F-labeled small molecules, the construction of radiometallated antibodies, and the creation of pretargeted imaging systems.

  10. Special Issue Articles

    1. Top of page
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    1. Bioorthogonal chemistry for 68Ga radiolabelling of DOTA-containing compounds (pages 291–297)

      Helen L. Evans, Laurence Carroll, Eric O. Aboagye and Alan C. Spivey

      Version of Record online: 5 DEC 2013 | DOI: 10.1002/jlcr.3153

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      Bioorthogonal reactions, which do not perturb or interfere with biological systems and are characterised by fast reaction kinetics, may be useful tools for radiolabelling biomolecules via a two-step labelling procedure. Here, we demonstrate a series of bioorthogonal radiochemistry reactions using 68Ga-DOTA labelled prosthetic groups, highlighting the versatility of this approach for potential imaging applications.

  11. Special Issue Reviews

    1. Top of page
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    1. You have full text access to this OnlineOpen article
      Potential clinical applications of bimodal PET-MRI or SPECT-MRI agents (pages 298–303)

      Rafael T. M. de Rosales

      Version of Record online: 7 JAN 2014 | DOI: 10.1002/jlcr.3154

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      The introduction to the clinic of positron emission tomography-magnetic resonance imaging scanners opens up the possibility to evaluate the real potential of bimodal imaging agents. In this mini-review, the limitations in the design and applications of these materials are summarised and the unique properties that may result in real clinical applications outlined.

    2. Radiolabelled porphyrins in nuclear medicine (pages 304–309)

      Philip A. Waghorn

      Version of Record online: 19 DEC 2013 | DOI: 10.1002/jlcr.3166

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      This review describes the approaches and advances in the preparation and use of radiolabelled porphyrin agents for imaging and therapeutic applications in nuclear medicine.

    3. Imaging the inside of a tumour: a review of radionuclide imaging and theranostics targeting intracellular epitopes (pages 310–316)

      Bart Cornelissen

      Version of Record online: 7 JAN 2014 | DOI: 10.1002/jlcr.3152

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      Imaging and molecular therapy of intracellular and intranuclear targets: a review.

    4. Imaging COX-2 expression in cancer using PET/SPECT radioligands: current status and future directions (pages 317–322)

      A. Pacelli, J. Greenman, C. Cawthorne and G. Smith

      Version of Record online: 18 DEC 2013 | DOI: 10.1002/jlcr.3160

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      Radiolabelled cyclooxygenase-2 probes have been the focus of considerable interest over the last few years, but progress to optimal imaging agents has been slow. This is in large part a result of the challenging nature of the target and the local tumour microenvironment. This review summarises the most recent developments in the area.

    5. Alternative approaches for PET radiotracer development in Alzheimer's disease: imaging beyond plaque (pages 323–331)

      Jason P. Holland, Steven H. Liang, Benjamin H. Rotstein, Thomas L. Collier, Nickeisha A. Stephenson, Ivan Greguric and Neil Vasdev

      Version of Record online: 11 DEC 2013 | DOI: 10.1002/jlcr.3158

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      Developing new positron-emitting radiotracers for imaging changes in signaling pathways associated with the pathobiology of AD is crucial to advancing our understanding of the disease and in aiding the evaluation of potential treatments. In this brief review, we present the chemical basis of various radiotracers which show promise in either preclinical or clinical studies for use in studying AD.

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