Differences in Accumulation and the Transport Mechanism of l- and d-Methionine in High- and Low-Grade Human Glioma Cells
Although [S-methyl-11C]-labeled L- and D-methionine (11C-L- and 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 11C-D-MET and 11C-L-MET are the same. 11C-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. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - September 13, 2016 Category: Nuclear Medicine Authors: Masato Kobayashi, Asuka Mizutani, Kodai Nishi, Syuichi Nakajima, Naoto Shikano, Ryuichi Nishii, Kazuki Fukuchi, Keiichi Kawai Source Type: research

New potent A1 adenosine receptor radioligands for positron emission tomography
8-Cyclopentyl-3-(3-[18F]fluoropropyl)-1-propylxanthine ([18F]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. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - September 12, 2016 Category: Nuclear Medicine Authors: Sabrina Kreft, Dirk Bier, Marcus H. Holschbach, Annette Schulze, Heinz H. Coenen Source Type: research

Impact of benzodiazepines on brain FDG-PET quantification after single-dose and chronic administration in rats
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. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - September 9, 2016 Category: Nuclear Medicine Authors: Jes ús 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 Source Type: research

Inhibition of viability of microorganisms in [18F]-labelled radiopharmaceuticals
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 sterilisation of the product is not always possible due to short half-life or due to thermal instability of the compound. The typical method for sterilisation in these cases is sterile filtration prior to dispensing (distribution of product solution from bulk to patient vials). (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - September 9, 2016 Category: Nuclear Medicine Authors: G. J örg, M. Fosselmann, W. Leis, F. Oberdorfer, Ch. Fehsenfeld Source Type: research

Corrigendum to “Cardiovascular side-effects and insulin secretion after intravenous administration of radiolabeled Exendin-4 in pigs” [Nucl Med Biol 43 (2016) 397–402]
The authors regret the omission of co-author Irina Velikyan (Section of Nuclear Medicine and PET, Department of Surgical Sciences, Uppsala University, Uppsala, Sweden). The authors would like to apologize for any inconvenience caused. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - September 6, 2016 Category: Nuclear Medicine Authors: Anneli Ryd én, Görel Nyman, Lovisa Nalin, Susanne Andreasson, Olle Korsgren, Olof Eriksson, Marianne Jensen-Waern Tags: Corrigendum Source Type: research

Commentary
Happy New Year and thank you for your continued support of Nucl Med Biol. Over the years, Nucl Med Biol has published commentaries and reviews addressing validation of targeted radiotracers with the goal of better understanding human biology or improving patient care through diagnosis or radiotherapy. These are based on the Aims and Scope of Nucl Med Biol (http://www.journals.elsevier.com/nuclear-medicine-and-biology). (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - September 2, 2016 Category: Nuclear Medicine Source Type: research

Tactics for preclinical validation of receptor-binding radiotracers
Aspects of radiopharmaceutical development are illustrated through preclinical studies of [125I]-(E)-1-(2-(2,3-dihydrobenzofuran-5-yl)ethyl)-4-(iodoallyl)piperazine ([125I]-E-IA-BF-PE-PIPZE), a radioligand for sigma-1 ( σ1) receptors, coupled with examples from the recent literature. Findings are compared to those previously observed for [125I]-(E)-1-(2-(2,3-dimethoxy-5-yl)ethyl)-4-(iodoallyl)piperazine ([125I]-E-IA-DM-PE-PIPZE). (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - September 1, 2016 Category: Nuclear Medicine Authors: Susan Z. Lever, Kuo-Hsien Fan, John R. Lever Source Type: research

Evaluation of pancreatic VMAT2 binding with active and inactive enantiomers of 18F-FP-DTBZ in baboons
18F-Fluoropropyl-(+)-dihydrotetrabenazine (18F-FP-(+)-DTBZ) is a vesicular monoamine transporter type 2 (VMAT2) radiotracer for positron emission tomography (PET) imaging to quantify human β-cell mass. Renal cortex and spleen have been suggested as reference regions, however, little is known about 18F-FP-(+)-DTBZ binding in these regions including the fraction of radiometabolite. We compared the kinetics of 18F-FP-(+)-DTBZ and its inactive enantiomer 18F-FP-(−)-DTBZ in baboons, est imated the non-displaceable binding (VND) of the tracers, and used ex vivo studies to measure radiometabolite fractions. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 31, 2016 Category: Nuclear Medicine Authors: Mika Naganawa, Shu-fei Lin, Keunpoong Lim, David Labaree, Jim Ropchan, Paul Harris, Yiyun Huang, Masanori Ichise, Richard E. Carson, Gary W. Cline Source Type: research

Nuclear data for production and medical application of radionuclides: Present status and future needs
The significance of nuclear data in the choice and medical application of a radionuclide is considered: the decay data determine its suitability for organ imaging or internal therapy and the reaction cross section data allow optimisation of its production route. A brief discussion of reaction cross sections and yields is given. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 31, 2016 Category: Nuclear Medicine Authors: Syed M. Qaim Source Type: research

Monooxorhenium(V) complexes with 222-N2S2 MAMA ligands for bifunctional chelator agents: Syntheses and preliminary in vivo evaluation
Targeted radiotherapy using the bifunctional chelate approach with 186/188Re(V) is challenging because of the susceptibility of monooxorhenium(V)-based complexes to oxidize in vivo at high dilution. A monoamine-monoamide dithiol (MAMA)-based bifunctional chelating agent was evaluated with both rhenium and technetium to determine its utility for in vivo applications. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 29, 2016 Category: Nuclear Medicine Authors: Dustin Wayne Demoin, Ashley N. Dame, William D. Minard, Fabio Gallazzi, Gary L. Seickman, Tammy L. Rold, Nicole Bernskoetter, Michael E. Fassbender, Timothy J. Hoffman, Carol A. Deakyne, Silvia S. Jurisson Source Type: research

Melanoma targeting with [99mTc(N)(PNP3)]-labeled α-melanocyte stimulating hormone peptide analogs: effects of cyclization on the radiopharmaceutical properties
The purpose of this study was to evaluate the effect of cyclization on the biological profile of a [99mTc(N)(PNP3)]-labeled α-melanocyte stimulating hormone peptide analog. A lactam bridge-cyclized H-Cys-Ahx-βAla3-c[Lys4-Glu-His-D-Phe-Arg-Trp-Glu10]-Arg11-Pro-Val-NH2 (NAP―NS2) and the corresponding linear H-Cys-Ahx-βAla-Nle-Asp-His-D-Phe-Arg-Trp-Gly-NH2 (NAP―NS1) peptide were synthetized, characterized by ESI-MS s pectroscopy and their melanocortin-1 receptor (MC1R) binding affinity was determined in B16/F10 melanoma cells. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 29, 2016 Category: Nuclear Medicine Authors: Davide Carta, Nicola Salvarese, Nicol ò Morellato, Feng Gao, Wiebke Sihver, Hans Jurgen Pietzsch, Barbara Biondi, Paolo Ruzza, Fiorenzo Refosco, Debora Carpanese, Antonio Rosato, Cristina Bolzati Source Type: research

On the applicability of [18F]FBPA to predict L-BPA concentration after amino acid preloading in HuH-7 liver tumor model and the implication for liver boron neutron capture therapy
In recent years extra-corporal application of Boron Neutron Capture Therapy (BNCT) was evaluated for liver primary tumors or liver metastases. A prerequisite for such a high-risk procedure is proof of preferential delivery and high uptake of a 10B-pharmaceutical in liver malignancies. In this work we evaluated in a preclinical tumor model if [18F]FBPA tissue distribution measured with PET is able to predict the tissue distribution of [10B]L-BPA. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 28, 2016 Category: Nuclear Medicine Authors: Catrin Grunewald, Michael Sauberer, Thomas Filip, Thomas Wanek, Johann Stanek, Severin Mairinger, Sofia Rollet, Petra Kudejova, Oliver Langer, Christian Sch ütz, Matthias Blaickner, Claudia Kuntner Source Type: research

Facile Room Temperature Synthesis of Fluorine-18 Labeled Fluoronicotinic acid-2,3,5,6-Tetrafluorophenyl Ester without Azeotropic Drying of Fluorine-18
Fluorine-18 labeled fluoronicotinic acid-2,3,5,6-tetrafluorophenyl ester has been successfully synthesized in an unprecedented way by flowing an acetonitrile solution of its quaternary ammonium salt precursor (N,N,N-trimethyl-5-((2,3,5,6-tetrafluorophenoxy)carbonyl)pyridin-2-aminium trifluoromethanesulfonate, 1) through an anion exchange cartridge. The fluorination reaction proceeded at room temperature without azeotropic drying of the fluoride. Over 75% conversion was observed with 10mg of precursor in 2:8, acetonitrile: t-butanol in 1min. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 28, 2016 Category: Nuclear Medicine Authors: Falguni Basuli, Xiang Zhang, Elaine M. Jagoda, Peter L. Choyke, Rolf E. Swenson Source Type: research

Copper-64 Labeled Liposomes for Imaging Bone Marrow
Bone marrow is the soft tissue compartment inside the bones made up of hematopoietic cells, adipocytes, stromal cells, phagocytic cells, stem cells, and sinusoids. While [18F]-FLT has been utilized to image proliferative marrow, to date, there are no reports of particle based positron emission tomography (PET) imaging agents for imaging bone marrow. We have developed copper-64 labeled liposomal formulation that selectively targets bone marrow and therefore serves as an efficient PET probe for imaging bone marrow. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 26, 2016 Category: Nuclear Medicine Authors: Sang-gyu Lee, Kishore Gangangari, Teja Muralidhar Kalidindi, Blesida Punzalan, Steven M. Larson, Naga Vara Kishore Pillarsetty Source Type: research

111In-Labeled Trastuzumab-Modified Gold Nanoparticles are Cytotoxic In Vitro to HER2-Positive Breast Cancer Cells and Arrest Tumor Growth In Vivo in Athymic Mice After Intratumoral Injection
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, 111In (trastuzumab-AuNP-111In). Our objective was to determine the cytotoxicity of trastuzumab-AuNP-111In on HER2-positive BC cells in vitro and evaluate its tumor growth-inhibition properties and normal tissue toxicity in vivo following intratumoral (i.t.) injection in mice with s.c. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 22, 2016 Category: Nuclear Medicine Authors: Zhongli Cai, Niladri Chattopadhyay, Kaiyu Yang, Yongkyu Luke Kwon, Simmyung Yook, Jean-Philippe Pignol, Raymond M. Reilly Source Type: research