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Nuclear Medicine and Biology

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https://www.readbyqxmd.com/read/30390575/tumor-uptake-and-tumor-blood-ratios-for-89-zr-dfo-trastuzumab-dm1-on-micropet-ct-images-in-nod-scid-mice-with-human-breast-cancer-xenografts-are-directly-correlated-with-her2-expression-and-response-to-trastuzumab-dm1
#1
Noor Al-Saden, Zhongli Cai, Raymond M Reilly
INTRODUCTION: Our objective was to determine correlations between the tumor uptake and T/B ratios for 89 Zr-labeled T-DM1 (89 Zr-DFO-T-DM1) in mice with human BC xenografts by microPET/CT and biodistribution studies with HER2 expression and response to treatment with trastuzumab-DM1 (T-DM1). METHODS: The tumor and normal tissue uptake and T/B ratios for 89 Zr-DFO-T-DM1 (10 μg; 7.0 MBq) incorporated into a therapeutic dose (60 μg) were determined by microPET/CT and biodistribution studies at 96 h p...
October 16, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30388434/al-18-f-complexation-of-dfh17-a-nota-conjugated-adrenomedullin-analog-for-pet-imaging-of-pulmonary-circulation
#2
Luis Michel Alonso Martinez, François Harel, Quang T Nguyen, Myriam Létourneau, Caroline D'Oliviera-Sousa, Bernard Meloche, Vincent Finnerty, Alain Fournier, Jocelyn Dupuis, Jean N DaSilva
INTRODUCTION: Adrenomedullin receptors are highly expressed in human alveolar capillaries and provide a molecular target for imaging the integrity of pulmonary microcirculation. In this work, we aimed to develop a NOTA-derivatized adrenomedullin analog (DFH17), radiolabeled with [18 F]AlF, for PET imaging of pulmonary microcirculation. METHODS: Highly concentrated [18 F](AlF)2+ (15 μL) was produced from purified fluorine-18 in NaCl 0.9%. Various complexation experiments were carried out at Al-to-NOTA molar ratios ranging from 1:1 to 1:40 to assess optimal radiolabeling conditions before using the peptide...
October 16, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30380462/unexpected-decrease-in-in-vivo-binding-of-3-h-qnb-in-the-mouse-cerebral-cortex-in-the-developing-brain-a-comparison-with-11-c-nmpb
#3
Osamu Inoue, Toshiyuki Sato, Kaoru Kobayashi, Antony Gee, Miho Shukuri, Ming-Rong Zhang
INTRODUCTION: Significant discrepancies between in vitro and in vivo binding of the muscarinic receptor ligand - 3 H-labeled Quinuclidinyl Benzilate (QNB) - have been well documented. Discernable in vivo cerebellar [3 H]QNB binding has been observed in mouse brain, despite the maximum number of binding sites (Bmax ) being low. In order to understand this unique in vivo binding phenomenon, the binding of two muscarinic receptor ligands - [3 H]QNB and N-[11 C]methylpiperidyl Benzilate ([11 C]NMPB) - were compared in vivo and in vitro in 3- and 8-week-old mice...
October 16, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30380464/efficient-cartridge-purification-for-producing-high-molar-activity-18-f-glycoconjugates-via-oxime-formation
#4
Outi Keinänen, Denisa Partelová, Osku Alanen, Maxim Antopolsky, Mirkka Sarparanta, Anu J Airaksinen
INTRODUCTION: 18 F-fluoroglycosylation via oxime formation is a chemoselective and mild radiolabeling method for sensitive molecules. Glycosylation can also improve the bioavailability, in vivo kinetics, and stability of the compound in blood, as well as accelerate clearance of biomolecules. A typical synthesis procedure for 18 F-fluoroglycosylation with [18 F]FDG (2-deoxy-2-[18 F]fluoro-d-glucose) and [18 F]FDR (5-deoxy-5-[18 F]fluoro-d-ribose) involves two HPLC (high performance liquid chromatography) purifications: one after 18 F-fluorination of the carbohydrate to remove its labeling precursor, and a second one after the oxime formation step to remove the aminooxy precursor...
October 15, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30359787/automated-radiosynthesis-of-5-11-c-l-glutamine-an-important-tracer-for-glutamine-utilization
#5
Adam J Rosenberg, Michael L Nickels, Michael L Schulte, H Charles Manning
INTRODUCTION: The natural amino acid l-Glutamine (Gln) is essential for both cell growth and proliferation. In addition to glucose, cancer cells utilize Gln as a carbon source for ATP production, biosynthesis, and as a defense against reactive oxygen species. The utilization of [11 C]Gln has been previously reported as a biomarker for tissues with an elevated demand for Gln, however, the previous reports for the preparation of [11 C]Gln were found to be lacking several crucial aspects necessary for transition to human production...
October 15, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30380463/molar-activity-the-keystone-in-11-c-radiochemistry-an-explorative-study-using-the-gas-phase-method
#6
Verena Pichler, Thomas Zenz, Cécile Philippe, Chrysoula Vraka, Neydher Berrotéran-Infante, Sarah Pfaff, Lukas Nics, Marius Ozenil, Oliver Langer, Matthäus Willeit, Tatjana Traub-Weidinger, Rupert Lanzenberger, Markus Mitterhauser, Marcus Hacker, Wolfgang Wadsak
INTRODUCTION: Radiochemists/radiopharmacists, involved in the preparation of radiopharmaceuticals are regularly confronted with the requirement of continuous high quality productions in their day-to-day business. One of these requirements is high specific or molar activity of the radiotracer in order to avoid e.g. receptor saturation and pharmacological or even toxic effects of the applied tracer for positron emission tomography. In the case of 11 C-labeled radiotracers, the reasons for low molar activity are manifold and often the search for potential 12 C-contaminations is time-consuming...
October 12, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30317069/-18-f-f-dpa-for-the-detection-of-activated-microglia-in-a-mouse-model-of-alzheimer-s-disease
#7
Thomas Keller, Francisco R López-Picón, Anna Krzyczmonik, Sarita Forsback, Anna K Kirjavainen, Jatta S Takkinen, Obada Alzghool, Johan Rajander, Simo Teperi, Fanny Cacheux, Annelaure Damont, Frédéric Dollé, Juha O Rinne, Olof Solin, Merja Haaparanta-Solin
INTRODUCTION: Neuroinflammation is associated with several neurological disorders, including Alzheimer's disease (AD). The translocator protein 18 kDa (TSPO), due to its overexpression during microglial activation and relatively low levels in the brain under normal neurophysiological conditions, is commonly used as an in vivo biomarker for neuroinflammation. Reported here is the preclinical evaluation of [18 F]F-DPA, a promising new TSPO-specific radioligand, as a tool for the detection of activated microglia at different ages in the APP/PS1-21 mouse model of AD and a blocking study to determine the specificity of the tracer...
September 26, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30209016/issues-in-preclinical-radiopharmaceutical-research-significance-relevance-and-reproducibility
#8
EDITORIAL
Michael R Kilbourn, Peter J H Scott
No abstract text is available yet for this article.
September 3, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30208358/assessing-the-feasibility-of-intranasal-radiotracer-administration-for-in-brain-pet-imaging
#9
Nisha Singh, Mattia Veronese, Jim O'Doherty, Teresa Sementa, Salvatore Bongarzone, Diana Cash, Camilla Simmons, Marco Arcolin, Paul K Marsden, Antony Gee, Federico E Turkheimer
INTRODUCTION: The development of clinically useful tracers for PET imaging is enormously challenging and expensive. The intranasal (IN) route of administration is purported to be a viable route for delivering drugs to the brain but has, as yet, not been investigated for the delivery of PET tracers. If the intranasal (IN) pathway presents a viable option, it extends the PET imaging field by increasing the number of tracers available for human use. Here we report the results of a rodent study testing the feasibility of the IN route to administer radiotracers for brain PET imaging...
August 30, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30257223/dynamic-tspo-pet-for-assessing-early-effects-of-cerebral-hypoxia-and-resuscitation-in-new-born-pigs
#10
Charlotte de Lange, Rønnaug Solberg, Jon Erik Holtedahl, Andreas Tulipan, Jon Barlinn, William Trigg, Torild Wickstrøm, Ola Didrik Saugstad, Eirik Malinen, Mona Elisabeth Revheim
INTRODUCTION: Inflammation associated with microglial activation may be an early prognostic indicator of perinatal hypoxic ischemic injury, where translocator protein (TSPO) is a known inflammatory biomarker. This piglet study used dynamic TSPO-PET with [18 F]GE180 to evaluate if microglial activation after global perinatal hypoxic injury could be detected. METHODS: New born anesthetized pigs (n = 14) underwent hypoxia with fraction of inspired oxygen (FiO2 )0...
August 24, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30195072/preliminary-evaluation-of-a-novel-18-f-labeled-parp-1-ligand-for-pet-imaging-of-parp-1-expression-in-prostate-cancer
#11
Dong Zhou, Jinbin Xu, Cedric Mpoy, Wenhua Chu, Sung Hoon Kim, Huifangjie Li, Buck E Rogers, John A Katzenellenbogen
INTRODUCTION: Poly (ADP-ribose) polymerase-1 (PARP-1) plays many roles in prostate cancer (PC), such as mediating DNA damage repair, transcriptional regulation and nuclear hormone receptor signaling. Because of this, PARP-1 has been targeted for therapy in PC, and non-invasive imaging of PARP-1 could help predict which patients are likely to respond to such therapy. Several PARP-1 positron emission tomography (PET) imaging agents have been developed and show promise for imaging PARP-1 expression in breast, brain, and lung cancer in small animals, but not as yet in prostate cancer...
August 24, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30015090/evaluation-of-a-chloride-based-89-zr-isolation-strategy-using-a-tributyl-phosphate-tbp-functionalized-extraction-resin
#12
Stephen A Graves, Christopher Kutyreff, Kendall E Barrett, Reinier Hernandez, Paul A Ellison, Steffen Happel, Eduardo Aluicio-Sarduy, Todd E Barnhart, Robert J Nickles, Jonathan W Engle
INTRODUCTION: The remarkable stability of the 89 Zr-DOTA complex has been shown in recent literature. The formation of this complex appears to require 89 Zr-chloride as the complexation precursor rather than the more conventional 89 Zr-oxalate. In this work we present a method for the direct isolation of 89 Zr-chloride from irradiated nat Y foils. METHODS: 89 Zr, 88 Zr, and 88 Y were prepared by 16 MeV proton irradiation of nat Y foils and used for batch-extraction based equilibrium coefficient measurements for TBP and UTEVA resin...
September 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30248568/synthesis-and-evaluation-of-an-n-18-f-fluorodeoxyglycosyl-amino-acid-for-pet-imaging-of-tumor-metabolism
#13
Zhifang Wu, Jingxin Ma, Anna-Liisa Brownell, Hongliang Wang, Chaomin Li, Xiaxia Meng, Ling Yuan, Haiyan Liu, Sijin Li, Jun Xie
INTRODUCTION: The limitations of [18 F]fluorodeoxyglucose ([18 F]FDG), including producing false-positive or -negative results, low image contrast in brain tumor diagnosis and poor differentiation of tumor and inflammatory, necessitate the development of new radiopharmaceuticals. In the present study, a novel [18 F]fluoroglycoconjugate tracer, [18 F]FDGly-NH-Phe, for tumor metabolism imaging was prepared and evaluated. METHODS: [18 F]FDGly-NH-Phe was prepared by condensing [18 F]FDG with L-4-aminophenylalanine in an acidic condition, and purified with semi-preparative-high performance liquid chromatography (HPLC)...
August 16, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30170197/-99m-tc-duramycin-a-potential-molecular-probe-for-early-prediction-of-tumor-response-after-chemotherapy
#14
Yi Li, Cheng Liu, Xiaoping Xu, Xiaoling Lu, Jianming Luo, Brian Gray, Koon Y Pak, Jingyi Cheng, Yingjian Zhang
OBJECTIVE: Apoptosis plays a crucial role in many biological processes, especially in cancer. However, real-time monitoring of apoptosis is challenging. [99m Tc]duramycin can selectively target an apoptosis biomarker: phosphatidylethanolamine (PE), which is normally located on the intracellular cell-membrane surface but redistributes onto the outer cell-membrane upon apoptosis. Therefore, 99m Tc-duramycin is a potential probe for non-invasive detection of apoptosis in real-time. The aim of this study was to evaluate the value of [99m Tc]duramycin for detecting early apoptotic response in tumors after chemotherapy, thus providing a tool for early prediction of curative effects in tumors...
August 9, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30170196/effects-of-adding-an-albumin-binder-chain-on-177-lu-lu-dotatate
#15
Etienne Rousseau, Joseph Lau, Zhengxing Zhang, Carlos F Uribe, Hsiou-Ting Kuo, Chengcheng Zhang, Jutta Zeisler, Nadine Colpo, Kuo-Shyan Lin, François Bénard
INTRODUCTION: [177 Lu]Lu-DOTATATE peptide receptor radionuclide therapy is used for treatment of neuroendocrine tumours. We investigated whether prolonging blood residence time of [177 Lu]Lu-DOTATATE with albumin binders could increase tumour accumulation and tumour-to-kidney ratios for improved therapeutic efficacy. METHODS: DOTATATE and its derivatives with an albumin-binder motif (GluAB-DOTATATE and AspAB-DOTATATE) were prepared by solid-phase peptide synthesis...
August 9, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30015093/one-pot-enzymatic-synthesis-of-l-3-11-c-lactate-for-pharmacokinetic-analysis-of-lactate-metabolism-in-rat-brain
#16
Takashi Temma, Hidekazu Kawashima, Naoya Kondo, Makoto Yamazaki, Kazuhiro Koshino, Hidehiro Iida
INTRODUCTION: Lactate could serve as an energy source and signaling molecule in the brain, although there is insufficient in vivo evidence to support this possibility. Here we aimed to use a one-pot enzymatic synthetic procedure to synthesize l-[3-11 C]lactate that can be used to evaluate chemical forms in the blood after intravenous administration, and as a probe for pharmacokinetic analysis of lactate metabolism in in vivo positron emission tomography (PET) scans with normal and fasted rats...
July 7, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30041148/preclinical-study-of-an-18-f-labeled-glutamine-derivative-for-cancer-imaging
#17
Cong Li, Hui Liu, Dongban Duan, Zhenhan Zhou, Zhibo Liu
INTRODUCTION: The emerging evidence that demonstrated the extra-demand of glutamine for cancer surviving strongly called for the development of PET tracer for imaging glutamine uptake in cancer. In this work, [18 F]Gln-BF3 as a natural glutamine derivative was synthesized to explore its potential application of imaging glutamine uptake for cancer diagnosis. METHODS: [18 F]Gln-BF3 was prepared by deprotection of purified precursor trityl-Gln-BF3 (amide bond protected with triphenylmethyl group) using TFA and radiolabeled using 18 F-19 F isotope exchange protocol...
July 6, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30056279/improving-metabolic-stability-of-fluorine-18-labeled-verapamil-analogs
#18
Renske M Raaphorst, Gert Luurtsema, Cindy J Schokker, Khaled A Attia, Robert C Schuit, Philip H Elsinga, Adriaan A Lammertsma, Albert D Windhorst
INTRODUCTION: Fluorine-18 labeled positron emission tomography (PET) tracers were developed to obtain more insight into the function of P-glycoprotein (P-gp) in relation to various conditions. They allow research in facilities without a cyclotron as they can be transported with a half-life of 110 min. As the metabolic stability of previously reported tracers [18 F]1 and [18 F]2 was poor, the purpose of this study was to improve this stability using deuterium substitution, creating verapamil analogs [18 F]1-d4 , [18 F]2-d4 , [18 F]3-d3 and [18 F]3-d7 ...
July 5, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/30096380/-18-f-diphenyl-sulfide-derivatives-for-imaging-serotonin-transporter-sert-in-the-brain
#19
Yan Zhang, Futao Liu, Hao Xiao, Xinyue Yao, Genxun Li, Seok Rye Choi, Karl Ploessl, Zhihao Zha, Lin Zhu, Hank F Kung
OBJECTIVES: Serotonin transporters (SERT) play an important role in controlling serotonin concentration in the synaptic cleft and in managing postsynaptic signal transduction. Inhibitors of SERT binding are well known as selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine, sertraline, paroxetine, and escitalopram, that are commonly prescribed antidepressants. Positron emission tomography (PET) and single photon emission tomography (SPECT) imaging agents targeting SERT may be useful for studying its function and providing a tool for monitoring drug treatment...
July 4, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29929115/matched-pair-86-y-90-y-labeled-bivalent-rgd-bombesin-antagonist-rgd-glu-do3a-6-ahx-rm2-as-a-potential-theranostic-agent-for-prostate-cancer
#20
Nilantha Bandara, Tamila J Stott Reynolds, Rebecca Schehr, Rajendra P Bandari, Philipp J Diebolder, Stephanie Krieger, Jingli Xu, Yubin Miao, Buck E Rogers, Charles J Smith
INTRODUCTION: In this study, we describe development of a true matched-pair theranostic agent that is able to target the αV β3 integrin and the gastrin releasing peptide receptor (GRPR). We herein describe methods to metallate and characterize the new conjugate and to validate its biological efficacy by in vitro and in vivo methods. METHODS: We have previously described the development of [RGD-Glu-6Ahx-RM2] (where RGD: Arg-Gly-Asp; Glu: glutamic acid; 6-Ahx: 6-amino hexanoic acid; RM2: (D-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2)) that has been conjugated to a DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) bifunctional chelating agent (BFCA) to afford [RGD-Glu-[DO3A]-6-Ahx-RM2] peptide...
July 2018: Nuclear Medicine and Biology
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