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Nuclear Medicine and Biology

Rubel Chakravarty, Sudipta Chakraborty, E R Radhakrishnan, Koramadai Kamaleshwaran, Ajit Shinto, Ashutosh Dash
INTRODUCTION: The commercially available (68)Ge/(68)Ga generators are generally used in clinical context in conjunction with automated or semi-automated modules for the syntheses of (68)Ga radiopharmaceuticals. It is desirable to develop strategies for the formulation of (68)Ga-radiopharmaceuticals without use of such expensive modules in order to make (68)Ga-based clinical positron emission tomography (PET) more popular and affordable worldwide. METHODS: An organic matrix based (68)Ge/(68)Ga generator was used for preparation of clinically relevant doses of four different (68)Ga-based radiopharmaceuticals, namely (68)Ga-DOTA-NOC, (68)Ga-NODAGA-RGD2, (68)Ga-PSMA-11 and (68)Ga-BPAMD...
November 16, 2016: Nuclear Medicine and Biology
Kun Hu, Shilpa Sonti, Sherrye T Glaser, Richard I Duclos, Samuel J Gatley
INTRODUCTION: 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 [(3)H-arachidonoyl]anandamide demonstrated deposition of tritium in thalamus and cortical areas that was blocked by treatment with an FAAH inhibitor and that was not seen in FAAH-knockout mice...
November 9, 2016: Nuclear Medicine and Biology
Wook Kim, Hyun Soo Park, Byung Seok Moon, Byung Chul Lee, Sang Eun Kim
INTRODUCTION: We measured the tiagabine-induced enhancement of the GABAA receptor's affinity for benzodiazepine ligands ("GABA shift") using [(18)F]flumazenil (FMZ) PET with preclinical application of bolus plus constant infusion (B/I). Differences in quantified results of [(18)F]FMZ binding were compared to that of [(18)F]FMZ PET with single bolus injection (SB). MATERIALS AND METHODS: Sprague-Dawley rats underwent [(18)F]FMZ PET scans with B/I, which consisted of baseline and "GABA shift" sessions in a scan, or scans with SB one week apart...
November 4, 2016: Nuclear Medicine and Biology
Ilinca Popp, Luigi Del Pozzo, Beatrice Waser, Jean Claude Reubi, Philipp T Meyer, Helmut R Maecke, Eleni Gourni
: 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 (64)Cu-CB-TE2A-AR06, (68)Ga-RM2 and (68)Ga-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...
November 4, 2016: Nuclear Medicine and Biology
Marc Pretze, Dominic Franck, Falk Kunkel, Erich Foßhag, Carmen Wängler, Björn Wängler
Two different strategies for the nucleophilic radiosynthesis of [(18)F]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 [(18)F]F-DOPA based on this strategy showed to be highly complex, giving the intermediate products as well as the final product in insufficient yields for automatization...
October 27, 2016: Nuclear Medicine and Biology
Jin-Young Paik, Kyung-Ho Jung, Jin-Hee Lee, Jin-Won Park, Kyung-Han Lee
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 (18)F-fluorodeoxyglucose ((18)F-FDG) uptake and lactate production. This was accompanied by augmented hexokinase activity and membrane Glut-1, and increased accumulation of hypoxia-inducible factor-1α (HIF1α). Restoration of oxygen reversed the metabolic effect, but this was blocked by HIF1α stabilization. Hypoxia-stimulated (18)F-FDG uptake was completely abrogated by silencing of HIF1α expression or by a specific inhibitor...
October 26, 2016: Nuclear Medicine and Biology
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
INTRODUCTION: 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 [(11)C]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...
October 26, 2016: Nuclear Medicine and Biology
Maroor Raghavan Ambikalmajan Pillai
No abstract text is available yet for this article.
October 18, 2016: Nuclear Medicine and Biology
Berend van der Wildt, Micha M M Wilhelmus, Esther J M Kooijman, Cornelis A M Jongenelen, Robert C Schuit, Christian Büchold, Ralf Pasternack, Adriaan A Lammertsma, Benjamin Drukarch, Albert D Windhorst
INTRODUCTION: The protein-protein crosslinking activity of the enzyme tissue transglutaminase (TG2; EC is associated with the pathogenesis of various diseases, including celiac disease, lung-, liver- and kidney fibrosis, cancer and neurodegenerative diseases. This study aims at developing a TG2 PET tracer based on the peptidic irreversible TG2 inhibitor Z006. METHODS: Initially, the carbon-11 labeling of Z006 at the diazoketone position was explored. Subsequently, a set of analogues that allow for fluorine-18 labeling was synthesized...
October 18, 2016: Nuclear Medicine and Biology
Hadis Honarvar, Cristina Müller, Susan Cohrs, Stephanie Haller, Kristina Westerlund, Amelie Eriksson Karlström, Nicholas P van der Meulen, Roger Schibli, Vladimir Tolmachev
INTRODUCTION: 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 (68)Ga (T½=68min) can visualize metastases of breast cancer expressing human epidermal growth factor receptor type 2 (HER2) and provide discrimination between tumors with high and low expression level. This may help to identify breast cancer patients benefiting from HER2-targeting therapies...
October 18, 2016: Nuclear Medicine and Biology
Fiorella Carla Tesan, Mariano Gastón Portillo, Marcela Analía Moretton, Ezequiel Bernabeu, Diego Andrés Chiappetta, Maria Jimena Salgueiro, Marcela Beatriz Zubillaga
INTRODUCTION: 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 (99m)Tc. METHODS: Labeling process was performed by a direct method...
September 30, 2016: Nuclear Medicine and Biology
Sébastien Schmitt, Jérôme Delamare, Olivier Tirel, Fabien Fillesoye, Martine Dhilly, Cécile Perrio
INTRODUCTION: 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. METHODS: Radiosynthesis of [(18)F]9 was achieved according to an automated two-step procedure from [(18)F]-fluoride. Peripheral and cerebral distributions were determined by ex vivo experiments and by PET imaging in mouse. Radiometabolism studies were performed both in vivo in mice and in vitro in mouse and human liver microsomes...
September 26, 2016: Nuclear Medicine and Biology
Masato Kobayashi, Asuka Mizutani, Kodai Nishi, Syuichi Nakajima, Naoto Shikano, Ryuichi Nishii, Kazuki Fukuchi, Keiichi Kawai
INTRODUCTION: Although [S-methyl-11C]-labeled L-methionine and D-methionine ((11)C-L-MET and (11)C-D-MET) are useful radiotracers for positron emission tomography imaging of brain tumors, it is not known whether the accumulation and transport mechanisms underlying uptake of (11)C-D-MET and (11)C-L-MET are the same. (11)C-L-MET is mainly taken up by the amino acid transport system L. We evaluated accumulation and the transport mechanism of D-MET in high- and low-grade human glioma cells in vitro...
September 14, 2016: Nuclear Medicine and Biology
Sabrina Kreft, Dirk Bier, Marcus H Holschbach, Annette Schulze, Heinz H Coenen
8-Cyclopentyl-3-(3-[(18)F]fluoropropyl)-1-propylxanthine ([(18)F]CPFPX) is meanwhile an accepted receptor ligand to examine the A1 adenosine receptor (A1AR) in humans by positron emission tomography (PET). A major drawback of this compound is its rather fast metabolic degradation in vivo. Therefore two new xanthine derivatives, namely 8-cyclobutyl-1-cyclopropymethyl-3-(3-fluoropropyl)xanthine (CBCPM; 5) and 1-cyclopropylmethyl-3-(3-fluoropropyl)-8-(1-methylcyclobutyl)xanthine (CPMMCB; 6) were designed and synthesized as potential alternatives to CPFPX...
September 13, 2016: Nuclear Medicine and Biology
G Jörg, M Fosselmann, W Leis, F Oberdorfer, Ch Fehsenfeld
INTRODUCTION: Good manufacturing practice (GMP)-compliant production of radiopharmaceuticals for parenteral application requires great efforts in maintenance of clean room infrastructure and equipment in order to reliably guarantee the constant hygienic quality of the product (sterility). Terminal sterilization of the product is not always possible due to short half-life or due to thermal instability of the compound. The typical method for sterilization in these cases is sterile filtration prior to dispensing (distribution of product solution from bulk to patient vials)...
September 10, 2016: Nuclear Medicine and Biology
Anneli Rydén, Görel Nyman, Lovisa Nalin, Susanne Andreasson, Olle Korsgren, Olof Eriksson, Marianne Jensen-Waern
No abstract text is available yet for this article.
September 7, 2016: Nuclear Medicine and Biology
Frederick O Cope, Bonnie Abbruzzese, James Sanders, Wendy Metz, Kristyn Sturms, David Ralph, Michael Blue, Jane Zhang, Paige Bracci, Wiam Bshara, Spencer Behr, Toby Maurer, Kenneth Williams, Joshua Walker, Allison Beverly, Brooke Blay, Anirudh Damughatla, Mark Larsen, Courtney Mountain, Erin Neylon, Kaeli Parcel, Kapil Raghuraman, Kevin Ricks, Lucas Rose, Akhilesh Sivakumar, Nicholas Streck, Bryan Wang, Christopher Wasco, Amifred Williams, Larry S Schlesinger, Abul Azad, Murugesan V S Rajaram, Wael Jarjour, Nicholas Young, Thomas Rosol, Michael McGrath
No abstract text is available yet for this article.
December 2016: Nuclear Medicine and Biology
Jesús Silva-Rodríguez, Lara García-Varela, Esteban López-Arias, Inés Domínguez-Prado, Julia Cortés, Juan Pardo-Montero, Anxo Fernández-Ferreiro, Álvaro Ruibal, Tomás Sobrino, Pablo Aguiar
INTRODUCTION: Current guidelines for brain PET imaging advice against the injection of diazepam prior to brain FDG-PET examination in order to avoid possible interactions of benzodiazepines with the radiotracer uptake. Nevertheless, many patients undergoing PET studies are likely to be under chronic treatment with benzodiazepines, for example due to the use of different medications such as sleeping pills. Animal studies may provide an extensive and accurate estimation of the effect of benzodiazepines on brain metabolism in a well-defined and controlled framework...
December 2016: Nuclear Medicine and Biology
Zhongli Cai, Niladri Chattopadhyay, Kaiyu Yang, Yongkyu Luke Kwon, Simmyung Yook, Jean-Philippe Pignol, Raymond M Reilly
INTRODUCTION: Gold nanoparticles (AuNP; 30nm) were modified with polyethylene glycol (PEG) chains linked to trastuzumab for binding to HER2-positive breast cancer (BC) cells and diethylenetriaminepentaacetic acid (DTPA) for complexing the Auger electron-emitter, (111)In (trastuzumab-AuNP-(111)In). Our objective was to determine the cytotoxicity of trastuzumab-AuNP-(111)In on HER2-positive BC cells in vitro and evaluate its tumor growth inhibition properties and normal tissue toxicity in vivo following intratumoral (i...
December 2016: Nuclear Medicine and Biology
David S Geller, Jonathan Morris, Ekaterina Revskaya, Mani Kahn, Wendong Zhang, Sajida Piperdi, Amy Park, Pratistha Koirala, Hillary Guzik, Charles Hall, Bang Hoang, Rui Yang, Michael Roth, Jonathan Gill, Richard Gorlick, Ekaterina Dadachova
INTRODUCTION: Osteosarcoma overall survival has plateaued around 70%, without meaningful improvements in over 30years. Outcomes for patients with overt metastatic disease at presentation or who relapse are dismal. In this study we investigated a novel osteosarcoma therapy utilizing radioimmunotherapy (RIT) targeted to IGF2R, which is widely expressed in OS. METHODS: Binding efficiency of the Rhenium-188((188)Re)-labeled IGF2R-specific monoclonal antibody (mAb) to IGF2R on OS17 OS cells was assessed with Scatchard plot analysis...
December 2016: Nuclear Medicine and Biology
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