Journal of Labelled Compounds and Radiopharmaceuticals

Cover image for Vol. 55 Issue 1

January 2012

Volume 55, Issue 1

Pages i–iv, 1–56

  1. Cover and Masthead

    1. Top of page
    2. Cover and Masthead
    3. Research Articles
    4. Technical Notes
    5. Notes
    1. Cover and Masthead (pages i–iv)

      Version of Record online: 25 JAN 2012 | DOI: 10.1002/jlcr.2905

  2. Research Articles

    1. Top of page
    2. Cover and Masthead
    3. Research Articles
    4. Technical Notes
    5. Notes
    1. Tritium labelling of PACAP-38 using a synthetic diiodinated precursor peptide (pages 1–4)

      Martin Holst Friborg Pedersen and Michael Baun

      Version of Record online: 3 NOV 2011 | DOI: 10.1002/jlcr.1941

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      In the interest of developing efficient methods for tritium labelling peptides, we here demonstrate the successful labelling of PACAP-38 (pituitary adenylate cyclase-activating polypeptide), a 38-mer peptide, using a synthetic diiodinated PACAP-38 precursor. In this example, we employ standard hydrogenation chemistry with the use of a heterogeneous palladium catalyst and carrier-free tritium gas on a tritium manifold system.

    2. Production and purification of the positron emitter zinc-63 (pages 5–9)

      Francisco L. Guerra Gómez, Yuuki Takada, Rie Hosoi, Sotaro Momosaki, Kazuhiko Yanamoto, Kotaro Nagatsu, Hisashi Suzuki, Ming-Rong Zhang, Osamu Inoue, Yasushi Arano and Toshimitsu Fukumura

      Version of Record online: 25 OCT 2011 | DOI: 10.1002/jlcr.1943

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      The positron emitting radionuclide 63Zn was produced from the irradiation of copper targets with protons. Short purification times were achieved by selective elution of zinc ions from cationic resins, and the final product was obtained in high chemical and radiochemical purities.

    3. Preparation and preliminary biological evaluation of 177Lu-labeled GluDTPA-cyclo(RGDfK) for integrin ανβ3 receptor-positive tumor targeting (pages 10–17)

      Jin-Hwan Kim, Jae-Cheong Lim, Ki-Cheol Yun, Sun-Ju Choi and Young-Don Hong

      Version of Record online: 25 NOV 2011 | DOI: 10.1002/jlcr.1944

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      In an attempt to develop RGD-based radiopharmaceutical, a novel GluDTPA-cyclo(RGDfK) possessing eight coordination sites was synthesized and radiolabeled with 177Lu as a model radionuclide. The 177Lu-labeled GluDTPA-cyclo(RGDfK) was formulated with a high yield (>98%) and sustained its radiochemical purity. The radiolabeled complex showed its proper biological affinity as a targeting agent for non-invasive imaging and detection of integrin ανβ3-positive tumors.

    4. Preparation of technetium-99m bifunctional chelate complexes using a microfluidic reactor: a comparative study with conventional and microwave labeling methods (pages 18–22)

      Ryan W. Simms, Patrick W. Causey, Darren M. Weaver, Chitra Sundararajan, Karin A. Stephenson and John F. Valliant

      Version of Record online: 25 OCT 2011 | DOI: 10.1002/jlcr.1946

      Thumbnail image of graphical abstract

      Microfluidic reactors enable higher radiochemical yields for labeling bifunctional chelates and a protein conjugate with technetium-99m relative to similarly formulated conventional methods.

    5. Temperature effects on the stereospecificity of nucleophilic fluorination: formation of trans-[18F]4-fluoro-l-proline during the synthesis of cis-[18F]4-fluoro-l-proline (pages 23–28)

      Babak Behnam Azad, Rezwan Ashique, N. Renée Labiris and Raman Chirakal

      Version of Record online: 3 NOV 2011 | DOI: 10.1002/jlcr.1947

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      We report a stereospecific route for the radiofluorination of (2S,4R)-N-tert-butoxycarbonyl-4-(p-toluenesulfonyloxy)proline methyl ester to produce diastereomerically pure cis-4-[18F]fluoro-l-proline. This work illustrates the effect of temperature on stereospecificity of nucleophilic radiofluorination and proves it to be a determining factor in the production of diastereomerically pure products. Two hydrolysis routes are also discussed for the deprotection of the fluorinated intermediate, providing a critical analysis on the choice of acid or acid/base hydrolysis for production of diastereomerically pure cis-[18F]4-fluoro-l-proline.

    6. Large-scale preparation and labelling reactions of deuterated silanes (pages 29–38)

      Jesús Campos, Miguel Rubio, Ana C. Esqueda and Ernesto Carmona

      Version of Record online: 21 NOV 2011 | DOI: 10.1002/jlcr.1950

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      A gramme-scale catalytic synthesis of the deuterated silanes SiEt3D, SiMe2PhD and SiPh2D2 is reported, utilizing D2 (0.5 bar) as the hydrogen isotope source and low catalyst loadings (0.01 mol%). The catalytic activity that rhodium complex 1 exhibits also toward hydrosilylation reactions has allowed us to develop a simple and proficient one-flask, two-step procedure for the deuterosilylation of various ketones, aldehydes and α,β-unsaturated nitriles.

    7. Rapid radiosynthesis of [11C] and [14C]azelaic, suberic, and sebacic acids for in vivo mechanistic studies of systemic acquired resistance in plants (pages 39–43)

      Marcel Best, Andrew N. Gifford, Sung Won Kim, Ben Babst, Markus Piel, Frank Rösch and Joanna S. Fowler

      Version of Record online: 25 NOV 2011 | DOI: 10.1002/jlcr.1951

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      A rapid procedure was developed for labeling the plant signaling molecule, azelaic acid (1,9-nonandioic acid), and related acids with 11C or 14C. Labeling was in two steps via reaction of the bromonitrile with 11C or 14C-cyanide, respectively, followed by alkaline hydrolysis.

  3. Technical Notes

    1. Top of page
    2. Cover and Masthead
    3. Research Articles
    4. Technical Notes
    5. Notes
    1. Biosynthesis of glucose-d-13C6 from Hansenula polymorpha and methanol-13C (pages 44–47)

      Zhan-feng Liu, Zheng Ren, Da-gang Xu and Liang-jun Li

      Version of Record online: 4 OCT 2011 | DOI: 10.1002/jlcr.1935

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      A simple and effective method for synthesis of glucose-d-13C6 via two steps is described. Firstly, the α,α-trehalose-13C12 can be obtained by fermentation using the methylotrophic yeast Hansenula polymorpha with 99% abundance methanol-13C and then be hydrolysed to give glucose-d-13C6 with 98.5% abundance 13C.

  4. Notes

    1. Top of page
    2. Cover and Masthead
    3. Research Articles
    4. Technical Notes
    5. Notes
    1. Synthesis of tritium-labeled levetiracetam ((2S)-2-(2-oxopyrrolidin-1-yl)butanamide) with high specific activity (pages 48–51)

      Simone Hildenbrand, Younis Baqi and Christa E. Müller

      Version of Record online: 18 OCT 2011 | DOI: 10.1002/jlcr.1942

      Thumbnail image of graphical abstract

      A method for the preparation of [3H]levetiracetam with a high specific activity of 98 Ci/mmol (3.6 TBq/mmol) is described. The radioligand proved to be highly useful for the labeling of specific levetiracetam binding sites in rat brain membrane preparations.

    2. Recombinant fragment of an antibody tailored for direct radioiodination (pages 52–56)

      Juraj Sedláček, Milan Fábry, Irena Sieglová, Vlastimil Král, Bronislava Uhnáková, Marcela Múdra, Leo Kronrád, Agnieszka Sawicka, Renata Mikolajczak and Pavlína Řezáčová

      Version of Record online: 11 NOV 2011 | DOI: 10.1002/jlcr.1945

      Thumbnail image of graphical abstract

      This article presents the design and preparation of a single-chain variable fragment (scFv) of an antibody comprising an auxiliary polypeptide segment that is rich in tyrosine. This protein shows a higher capacity to bind iodine radionuclide, as compared with the parental scFv. The tyrosine-rich segment of the tailored protein is less hydrophobic (i.e. more solvent exposed) and can thus contribute to a redirection of the label from potentially sensitive scFv tyrosine residues.

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