Journal of Labelled Compounds and Radiopharmaceuticals

Cover image for Vol. 57 Issue 1

January 2014

Volume 57, Issue 1

Pages i–iv, 1–64

  1. Cover and Masthead

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

      Version of Record online: 22 JAN 2014 | DOI: 10.1002/jlcr.3118

  2. Research Articles

    1. Top of page
    2. Cover and Masthead
    3. Research Articles
    4. Protocols and Methods
    5. Notes
    1. Synthesis of [3α-3H] 17α-Hydroxy pregnenolone and [3α-3H] Pregnenolone (pages 1–11)

      Yuan Tian, Yang Hong, Samuel J. Bonacorsi, Aaron Balog and Sharon Gong

      Version of Record online: 24 OCT 2013 | DOI: 10.1002/jlcr.3114

      Thumbnail image of graphical abstract

      [3α-3H] 17α-hydroxy pregnenolone (1) was synthesized through a multiple step sequence. The presence of [3β-3H] isomer was identified then separated with chiralPAK AD-H column. [3α-3H] pregnenolone (2) was synthesized from commercial available 5-pregnen-3,20-dione in one step.

    2. Preparation and biological evaluation of 99mTcN-labeled pteroyl-lys derivative as a potential folate receptor imaging agent (pages 12–17)

      Yuan Chen, Hongjuan Guo, Fang Xie and Jie Lu

      Version of Record online: 23 SEP 2013 | DOI: 10.1002/jlcr.3116

      Thumbnail image of graphical abstract

      In order to develop a novel 99mTc-labeled FR imaging agent, a dithiocarbamate derivative, pteroyl-lys-DTC, was synthesized and radiolabeled with 99mTc through the [99mTcN]2+ intermediate in high yield. The 99mTcN complex was stable under physiological conditions. The results of biological evaluation indicated that 99mTcN-pteroyl-lys-DTC was able to target the FR-positive tumor cells and tissues specifically both in vitro and in vivo.

    3. Synthesis and preliminary evaluation of 2-arylhydroxyquinoline derivatives for tau imaging (pages 18–24)

      Tetsuro Tago, Shozo Furumoto, Nobuyuki Okamura, Ryuichi Harada, Yoichi Ishikawa, Hiroyuki Arai, Kazuhiko Yanai, Ren Iwata and Yukitsuka Kudo

      Version of Record online: 16 OCT 2013 | DOI: 10.1002/jlcr.3133

      Thumbnail image of graphical abstract

      A 11C-labeled THK-951 was prepared by N-methylation with [11C]MeOTf in good yields and showed excellent brain kinetics and binding to tau depositions in an Alzheimer's disease brain section, suggesting an availability of 11C-THK-951 as a tau imaging agent by positron emission tomography.

    4. Preparation of clinical-grade 89Zr-panitumumab as a positron emission tomography biomarker for evaluating epidermal growth factor receptor-targeted therapy (pages 25–35)

      Ling Wei, Jianfeng Shi, George Afari and Sibaprasad Bhattacharyya

      Version of Record online: 13 NOV 2013 | DOI: 10.1002/jlcr.3134

      Thumbnail image of graphical abstract

      A robust method has been developed to produce clinical-grade immuno-PET tracer 89Zr-panitumumab for optimizing epidermal growth factor receptor-targeted therapy and measuring treatment response after therapy. This article illustrates a step-by-step method for the production and the quality control tests of 89Zr-panitumumab for clinical use.

    5. 99mTc-Doxycycline hyclate: a new radiolabeled antibiotic for bacterial infection imaging (pages 36–41)

      Derya İlem-Özdemir, Makbule Asikoglu, Hayal Ozkilic, Ferda Yilmaz, Mine Hosgor-Limoncu and Semin Ayhan

      Version of Record online: 21 NOV 2013 | DOI: 10.1002/jlcr.3135

      Thumbnail image of graphical abstract

      The aim of the study was radiolabeled Doxycycline Hyclate (DOX) with 99mTc from a cold kit formulation and to performed gamma scintigraphy and biodistribution studies with newly developed radiopharmaceutical 99mTc-DOX. Based on the in vivo studies, 99mTc-DOK has a higher uptake in infected thigh muscle, which can be easily visualized by scintigraphic studies.

  3. Protocols and Methods

    1. Top of page
    2. Cover and Masthead
    3. Research Articles
    4. Protocols and Methods
    5. Notes
    1. The development of an automated and GMP compliant FASTlab™ Synthesis of [18F]GE-180; a radiotracer for imaging translocator protein (TSPO) (pages 42–48)

      Torild Wickstrøm, Alan Clarke, Ingvil Gausemel, Eric Horn, Karina Jørgensen, Imtiaz Khan, Dimitrios Mantzilas, Thanushan Rajanayagam, Dirk-Jan In 't Veld and William Trigg

      Version of Record online: 23 SEP 2013 | DOI: 10.1002/jlcr.3112

      Thumbnail image of graphical abstract

      The radiotracer [18F]GE-180 binds selectively and with high affinity to TSPO and can be used to measure neuroinflammation in a variety of disease states. A suitable process for the radiosynthesis of [18F]GE-180 that meets the requirements for clinical use has been established for the FASTlab™ synthesizer. The use of integrated on-cassette solid phase extraction purification instead of the cost-consuming and time-consuming HPLC purification results in a user friendly, robust, and GMP compliant process with a product of high chemical and radiochemical purity.

  4. Notes

    1. Top of page
    2. Cover and Masthead
    3. Research Articles
    4. Protocols and Methods
    5. Notes
    1. Influence of radiolytic-produced hydrogen peroxide on the stability of commercial kit 99mtechnetium-exametazime preparation (pages 49–52)

      Teresa Martinez, Elena Miñana, Tomás Chivato Martín-Falquina and Teodomiro Fuente

      Version of Record online: 10 SEP 2013 | DOI: 10.1002/jlcr.3113

      Thumbnail image of graphical abstract

      99mTc-d,l- HMPAO is a widely used radiopharmaceutical that suffers from an inherent instability that constrains its availability for clinical use.

      A protocol for improving the stability of the kit with minimal modification of manufacturer's instructions and no chemicals addition to the commercial formulation is proposed. The protocol is based on the displacement of the oxygen present in the preparation, preventing free radicals build up and free pertechnetate formation, even when labelling with higher 99mTc pertechnetate quantities is required.

    2. Evaluation of the efficiency of Pd/H2-catalyzed benzylic H/D exchange of dehydroabietinal with D2O and synthesis of a tritium-labeled analogue (pages 53–56)

      Robby A. Petros and Jyoti Shah

      Version of Record online: 23 SEP 2013 | DOI: 10.1002/jlcr.3117

      Thumbnail image of graphical abstract

      Pd/H2-catalyzed exchange of benzylic hydrogen atoms of dehydroabietinal (DA) with 2H-H2O or 3H-H2O was conducted with >97% label incorporation for 2H-DA and a specific activity of 12.6 mCi/mmol for 3H-DA. The extent of deuterium labeling at each benzylic position was determined via an inverse-gated 13C NMR experiment. C7 and C15 were 87% and 81% labeled, respectively. Isotope-induced chemical shift changes at C6 were used to approximate the amount of singly (66%) and doubly (17%) labeled 2H-DA at C7.

    3. Syntheses of [3H2]T0901317 and a labeled structural isomer, and characterization of the dispersed labeled compounds via 19F NMR (pages 57–60)

      Benjamin P. Fauber, Adam R. Johnson, Stephen Bowerman, Brenda Burton, Adam Colebrook, Annerley Flynn, Gareth Harrold, Steve Huhn, Gary Jones, Peter Lockey, Maxine Norman, Olivier René and Harvey Wong

      Version of Record online: 26 NOV 2013 | DOI: 10.1002/jlcr.3138

      Thumbnail image of graphical abstract

      The synthesis and characterization of [3H2]T0901317 and a structural isomer are described. The structural assignments of the closely related labeled compounds were primarily accomplished via 19F NMR analyses of the corresponding ethanolic compound dispersions.

    4. Good manufacturing practice production of the system A amino acid transport tracer [11C]MeAIB on a commercial synthesis module (pages 61–64)

      Johan Hygum Dam and Kjell Någren

      Version of Record online: 26 NOV 2013 | DOI: 10.1002/jlcr.3139

      Thumbnail image of graphical abstract

      An automated good manufacturing practice process for the production of the system A amino acid transport tracer [11C]MeAIB on a commercial synthesis module has been established. Bioburden to the sterile filter was minimized during solid-phase extraction formulation of the HPLC purified product by the use of sterile aqueous solutions. The optimized solid-phase extraction formulation conditions are fast, give a high recovery of the product, and effectively remove organic solvents and adjust the pH.

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