Simvastatin augments revascularization and reperfusion in a murine model of hind limb ischemia – Multimodal imaging assessment
Peripheral artery disease can lead to severe disability and limb loss. Therapeutic strategies focussing on macrovascular repair have shown benefit but have not significantly reduced amputation rates in progressive PAD. Proangiogenic small molecule therapies may substantially improve limb vascularisation in limb ischemia. The purpose of the current study was to assess the proangiogenic effects of simvastatin in a murine model of hind limb ischemia using longitudinal multimodal imaging. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - November 16, 2016 Category: Nuclear Medicine Authors: JL Goggi, M Ng, N Shenoy, R Boominathan, P Cheng, S Sekar, KK Bhakoo Source Type: research
Clinical 68Ga-PET: Is Radiosynthesis Module an Absolute Necessity?
The commercially available 68Ge/68Ga generators are generally used in clinical context in conjunction with automated or semi-automated modules for the syntheses of 68Ga radiopharmaceuticals. It is desirable to develop strategies for the formulation of 68Ga-radiopharmaceuticals without use of such expensive modules in order to make 68Ga-based clinical positron emission tomography (PET) more popular and affordable worldwide. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - November 15, 2016 Category: Nuclear Medicine Authors: Rubel Chakravarty, Sudipta Chakraborty, E. Radhakrishnan, K.K. Kamaleshwaran, Ajit Shinto, Ashutosh Dash Source Type: research
Brain Uptake And Metabolism Of The Endocannabinoid Anandamide Labeled In Either The Arachidonoyl Or Ethanolamine Moiety
Anandamide (N-arachidonoylethanolamine) is a retrograde neuromodulator that activates cannabinoid receptors. The concentration of anandamide in the brain is controlled by fatty acid amide hydrolase (FAAH), which has been the focus of recent drug discovery efforts. Previous studies in C57BL/6 mice using [3H-arachidonoyl]anandamide demonstrated deposition of tritium in thalamus and cortical areas that was blocked by treatment with a FAAH inhibitor and that was not seen in FAAH-knockout mice. This suggested that long chain fatty acid amides radiolabeled in the fatty acid moiety might be useful as ex vivo and in vivo radiotrac...
Source: Nuclear Medicine and Biology - November 7, 2016 Category: Nuclear Medicine Authors: Kun Hu, Shilpa Sonti, Sherrye T Glaser, Richard I Duclos, Samuel J Gatley Source Type: research
Approaches to improve metabolic stability of a statine-based GRP receptor antagonist
The bombesin receptor family, in particular the gastrin-releasing peptide receptor (GRPr), is an attractive target in the field of nuclear oncology due to the high density of these receptors on the cell surface of several human tumors. The successful clinical implementation of 64Cu-CB-TE2A-AR06, 68Ga-RM2 and 68Ga-NODAGA-MJ9, prompted us to continue the development of GRPr-antagonists. The aim of the present study was to assess if N-terminal modulations of the statine-based GRPr-antagonist influence the binding affinity, the pharmacokinetic performance and the in vivo metabolic stability. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - November 2, 2016 Category: Nuclear Medicine Authors: Ilinca Popp, Luigi Del Pozzo, Beatrice Waser, Jean Claude Reubi, Philipp T. Meyer, Helmut R. Maecke, Eleni Gourni Source Type: research
PET measurement of “GABA shift” in the rat brain: a preclinical application of bolus plus constant infusion paradigm of [18F]flumazenil
We measured the tiagabine-induced enhancement of the GABAA receptor's affinity for benzodiazepine ligands ( “GABA shift”) using [18F]flumazenil (FMZ) PET with preclinical application of bolus plus constant infusion (B/I). Differences in quantified results of [18F]FMZ binding were compared to that of [18F]FMZ PET with single bolus injection (SB). (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - November 2, 2016 Category: Nuclear Medicine Authors: Wook Kim, Hyun Soo Park, Byung Seok Moon, Byung Chul Lee, Eun Kim Sang Source Type: research
Estimation of Radiation Dosimetry for 68Ga-HBED-CC (PSMA-11) in Patients with Suspected Recurrence of Prostate Cancer
This study was performed to estimate the human radiation dosimetry for [68Ga]Ga-HBED-CC (PSMA-11) (68Ga PSMA-11). Methods: Under an RDRC-approved research protocol, we evaluated the biodistribution and pharmacokinetics of 68Ga PSMA-11 with serial PET imaging following intravenous administration to nine prostate cancer patients in whom clinical [11C]acetate PET/CT exams had been independently performed under Expanded Access IND 118,204. List-mode imaging was performed over the initial 0 –10min post-injection with the pelvis in the field-of-view. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - November 2, 2016 Category: Nuclear Medicine Authors: Mark A. Green, Jacob A. Eitel, James W. Fletcher, Carla J. Mathias, Mark A. Tann, Thomas Gardner, Michael O. Koch, Wendy Territo, Heather Polson, Gary D. Hutchins Source Type: research
Re-assessing gallium-67 as a therapeutic radionuclide
Despite its desirable half-life and low energy Auger electrons that travel further than for other radionuclides, 67Ga has been neglected as a therapeutic radionuclide. Here, 67Ga is compared with Auger electron emitter 111In as a potential therapeutic radionuclide. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - October 28, 2016 Category: Nuclear Medicine Authors: Muhamad F. bin Othman, Nabil R. Mitry, Valerie J. Lewington, Philip J. Blower, Samantha Y.A. Terry Source Type: research
Evaluation of two nucleophilic syntheses routes for the automated synthesis of 6-[18F]Fluoro-l-DOPA
Two different strategies for the nucleophilic radiosynthesis of [18F]F-DOPA were evaluated regarding their applicability for an automated routine production on an Ecker&Ziegler Modular-Lab Standard module.Initially, we evaluated a promising 5-step synthesis based on a chiral, cinchonidine-derived phase-transfer catalyst (cPTC) being described to give the product in high radiochemical yields (RCY), high specific activities (AS) and high enantiomeric excesses (ee). However, the radiosynthesis of [18F]F-DOPA based on this strategy showed to be highly complex, giving the intermediate products as well as the final product in in...
Source: Nuclear Medicine and Biology - October 26, 2016 Category: Nuclear Medicine Authors: M. Pretze, D. Franck, F. Kunkel, E. Fo ßhag, C. Wängler, B. Wängler Source Type: research
A useful PET probe [11C]BU99008 with ultra-high specific radioactivity for small animal PET imaging of I2-imidazoline receptors in the hypothalamus
A positron emission tomography (PET) probe with ultra-high specific radioactivity (SA) enables measuring high receptor specific binding in brain regions by avoiding mass effect of the PET probe itself. It has been reported that PET probe with ultra-high SA can detect small change caused by endogenous or exogenous ligand. Recently, Kealey et al. developed [11C]BU99008, a more potent PET probe for I2-imidazoline receptors (I2Rs) imaging, with a conventional SA (mean 76GBq/ μmol) showed higher specific binding in the brain. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - October 25, 2016 Category: Nuclear Medicine Authors: Kazunori Kawamura, Yoko Shimoda, Joji Yui, Yiding Zhang, Tomoteru Yamasaki, Hidekatsu Wakizaka, Akiko Hatori, Lin Xie, Katsushi Kumata, Masayuki Fujinaga, Masanao Ogawa, Yusuke Kurihara, Nobuki Nengaki, Ming-Rong Zhang Source Type: research
Reactive oxygen species-driven HIF1 α triggers accelerated glycolysis in endothelial cells exposed to low oxygen tension
Endothelial cells and their metabolic state regulate glucose transport into underlying tissues. Here, we show that low oxygen tension stimulates human umbilical vein endothelial cell 18F-fluorodeoxyglucose (18F-FDG) uptake and lactate production. This was accompanied by augmented hexokinase activity and membrane Glut-1, and increased accumulation of hypoxia-inducible factor-1 α (HIF1α). Restoration of oxygen reversed the metabolic effect, but this was blocked by HIF1α stabilization. Hypoxia-stimulated 18F-FDG uptake was completely abrogated by silencing of HIF1α expression or by a specific inhibitor. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - October 25, 2016 Category: Nuclear Medicine Authors: Jin-Young Paik, Kyung-Ho Jung, Jin-Hee Lee, Jin-Won Park, Kyung-Han Lee Source Type: research
Development of fluorine-18 labelled peptidic PET tracers for imaging active tissue transglutaminase
This study aims at developing a TG2 PET tracer based on the peptidic irreversible TG2 inhibitor Z006. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - October 17, 2016 Category: Nuclear Medicine Authors: Berend van der Wildt, Micha M.M. Wilhelmus, Esther J.M. Kooijman, Cornelis A.M. Jongenelen, Robert C. Schuit, Christian B üchold, Ralf Pasternack, Adriaan A. Lammertsma, Benjamin Drukarch, Albert D. Windhorst Source Type: research
Evaluation of the first 44Sc-labeled Affibody molecule for imaging of HER2-expressing tumors
Affibody molecules are small (58 amino acids) high-affinity proteins based on a tri-helix non-immunoglobulin scaffold. A clinical study has demonstrated that PET imaging using Affibody molecules labeled with 68Ga (T ½=67.6min) can visualize metastases of breast cancer expressing human epidermal growth factor receptor type 2 and provide discrimination between tumors with high and low expression level. This may help to identify breast cancer patients benefiting from HER2-targeting therapies. The best discriminat ion was at 4h post injection. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - October 17, 2016 Category: Nuclear Medicine Authors: Hadis Honarvar, Cristina M üller, Susan Cohrs, Stephanie Haller, Kristina Westerlund, Amelie Eriksson Karlström, Nicholas P. van der Meulen, Roger Schibli, Vladimir Tolmachev Source Type: research
Preferred use of curie (Ci) rather than becquerel (Bq) in nuclear medicine practice
TO THE EDITOR: In 1975, the ‘15th Conférence Générale des Poids et Mesures’ adapted Becquerel as SI (The International System of Units, in French: Système international d'unités) unit of radioactivity through a resolution which stated - “…. by reason of the need to make as easy as possible the use of the units for non-specialists, taking into consideration also the grave risks of errors in therapeutic work, adopts the following special name for the SI unit of activity: becquerel, symbol Bq, equal to one reciprocal second” [1]. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - October 17, 2016 Category: Nuclear Medicine Authors: M.R.A. Pillai, F.F. (Russ) Knapp Source Type: research
Radiolabeling and Biological Characterization of TPGS-based Nanomicelles by Means of Small Animal Imaging
In recent years, nanomedicines have raised as a powerful tool to improve prevention, diagnosis and treatment of different pathologies. Among the most well investigated biomaterials, D- α-tocopheryl polyethylene glycol succinate (also known as TPGS) has been on the spot for the last decade. We therefore designed a method to biologically characterize TPGS-based nanomicelles by labeling them with 99mTc. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - September 29, 2016 Category: Nuclear Medicine Authors: Fiorella Carla Tesan, Mariano Gast ón Portillo, Marcela Analía Moretton, Ezequiel Bernabeu, Diego Andrés Chiappetta, Maria Jimena Salgueiro, Marcela Beatriz Zubillaga Source Type: research
N-[18F]-FluoropropylJDTic for κ-Opioid Receptor PET Imaging: Radiosynthesis, Pre-clinical Evaluation, and Metabolic Investigation in Comparison with Parent JDTic
To image kappa opioid receptor (KOR) for preclinical studies, N-fluoropropylJDTic 9 derived from the best-established KOR antagonist JDTic, was labeled with fluorine-18. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - September 25, 2016 Category: Nuclear Medicine Authors: S ébastien Schmitt, Jérôme Delamare, Olivier Tirel, Fabien Fillesoye, Martine Dhilly, Cécile Perrio Source Type: research
