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Nuclear Medicine and Biology

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https://www.readbyqxmd.com/read/28193503/clinical-translation-of-a-psma-inhibitor-for-99m-tc-based-spect
#1
Guillermina Ferro-Flores, Myrna Luna-Gutiérrez, Blanca Ocampo-García, Clara Santos-Cuevas, Erika Azorín-Vega, Nallely Jiménez-Mancilla, Emmanuel Orocio-Rodríguez, Jenny Davanzo, Francisco O García-Pérez
BACKGROUND: Prostate-specific membrane antigen (PSMA) is highly over-expressed in advanced prostate cancers. (68)Ga-labeled PSMA inhibitors (iPSMA) are currently used for prostate cancer detection by PET imaging. The availability of simple, efficient and reproducible radiolabeling procedures is essential for developing new SPECT radiopharmaceuticals for clinical translation. The aim of this research was to prepare (99m)Tc-EDDA/HYNIC-Lys(Nal)-Urea-Glu ((99m)Tc-EDDA/HYNIC-iPSMA) obtained from lyophilized kit formulations and evaluate the in vitro and in vivo radiopharmaceutical binding to prostate cancer cells over-expressing PSMA, as well as the (99m)Tc-EDDA/HYNIC-iPSMA normal biodistribution in humans and the preliminary uptake in patients with prostate cancer...
February 3, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28193502/development-of-a-preclinical-211-rn-211-at-generator-system-for-targeted-alpha-therapy-research-with-211-at
#2
Jason R Crawford, Hua Yang, Peter Kunz, D Scott Wilbur, Paul Schaffer, Thomas J Ruth
INTRODUCTION: The availability of (211)At for targeted alpha therapy research can be increased by the (211)Rn/(211)At generator system, whereby (211)At is produced by (211)Rn electron capture decay. This study demonstrated the feasibility of using generator-produced (211)At to label monoclonal antibody (BC8, anti-human CD45) for preclinical use, following isolation from the (207)Po contamination also produced by these generators (by (211)Rn α-decay). METHODS: (211)Rn was produced by (211)Fr electron capture decay following mass separated ion beam implantation and chemically isolated in liquid alkane hydrocarbon (dodecane)...
January 29, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28208058/monitoring-of-macrophage-accumulation-in-statin-treated-atherosclerotic-mouse-model-using-sodium-iodide-symporter-imaging-system
#3
Ran Ji Yoo, Min Hwan Kim, Sang-Keun Woo, Kwang Il Kim, Tae Sup Lee, Yang-Kyu Choi, Joo Hyun Kang, Sang Moo Lim, Yong Jin Lee
INTRODUCTION: Macrophages play a key role in atherosclerotic plaque formation in atherosclerosis, but its detailed understanding has poorly investigated until now. Thus, we sought to demonstrate a noninvasive technique for macrophage tracking to atherosclerotic lesions in apolipoprotein E(-/-)(ApoE(-/-)) mice with an imaging system based on sodium iodide symporter (NIS) gene coupled with (99m)Tc-single-photon emission computed tomography (SPECT). METHODS AND RESULTS: Macrophage cells (RAW264...
January 25, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28157625/iminodiacetic-acid-as-bifunctional-linker-for-dimerization-of-cyclic-rgd-peptides
#4
Dong Xu, Zuo-Quan Zhao, Shu-Ting Chen, Yong Yang, Wei Fang, Shuang Liu
INTRODUCTION: In this study, I2P-RGD2 was used as the example to illustrate a novel approach for dimerization of cyclic RGD peptides. The main objective of this study was to explore the impact of bifunctional linkers (glutamic acid vs. iminodiacetic acid) on tumor-targeting capability and excretion kinetics of the (99m)Tc-labeled dimeric cyclic RGD peptides. METHODS: HYNIC-I2P-RGD2 was prepared by reacting I2P-RGD2 with HYNIC-OSu in the presence of diisopropylethylamine, and was evaluated for its αvβ3 binding affinity against (125)I-echistatin bound to U87MG glioma cells...
January 20, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28160666/redesign-of-negatively-charged-111-in-dtpa-octreotide-derivative-to-reduce-renal-radioactivity
#5
Nobuhiro Oshima, Hiromichi Akizawa, Hidekazu Kawashima, Songji Zhao, Yan Zhao, Ken-Ichi Nishijima, Yoji Kitamura, Yasushi Arano, Yuji Kuge, Kazue Ohkura
INTRODUCTION: Radiolabeled octreotide derivatives have been studied as diagnostic and therapeutic agents for somatostatin receptor-positive tumors. To prevent unnecessary radiation exposure during their clinical application, the present study aimed to develop radiolabeled peptides which could reduce radioactivity levels in the kidney at both early and late post-injection time points by introducing a negative charge with an acidic amino acid such as L-aspartic acid (Asp) at a suitable position in (111)In-DTPA-conjugated octreotide derivatives...
January 17, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28126683/pet-imaging-of-64-cu-dota-scfv-anti-psma-lipid-nanoparticles-lnps-enhanced-tumor-targeting-over-anti-psma-scfv-or-untargeted-lnps
#6
Patty Wong, Lin Li, Junie Chea, Melissa K Delgado, Desiree Crow, Erasmus Poku, Barbara Szpikowska, Nicole Bowles, Divya Channappa, David Colcher, Jeffrey Y C Wong, John E Shively, Paul J Yazaki
INTRODUCTION: Single chain (scFv) antibodies are ideal targeting ligands due to their modular structure, high antigen specificity and affinity. These monovalent ligands display rapid tumor targeting but have limitations due to their fast urinary clearance. METHODS: An anti-prostate membrane antigen (PSMA) scFv with a site-specific cysteine was expressed and evaluated in a prostate cancer xenograft model by Cu-64 PET imaging. To enhance tumor accumulation, the scFv-cys was conjugated to the co-polymer DSPE-PEG-maleimide that spontaneously assembled into a homogeneous multivalent lipid nanoparticle (LNP)...
January 17, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28157626/evaluation-of-18-f-atri-as-pet-tracer-for-in-vivo-imaging-of-atr-in-mouse-models-of-brain-cancer
#7
Giuseppe Carlucci, Brandon Carney, Ahmad Sadique, Axel Vansteene, Jun Tang, Thomas Reiner
RATIONALE: Ataxia telangiectasia and Rad3-related (ATR) threonine serine kinase is one of the key elements in orchestrating the DNA damage response (DDR). As such, inhibition of ATR can amplify the effects of chemo- and radiation-therapy, and several ATR inhibitors (ATRi) have already undergone clinical testing in cancer. For more accurate patient selection, monitoring and staging, real-time in vivo imaging of ATR could be invaluable; the development of appropriate imaging agents has remained a major challenge...
January 16, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28104527/b7-h3-targeted-212-pb-radioimmunotherapy-of-ovarian-cancer-in-preclinical-models
#8
Benjamin B Kasten, Rebecca C Arend, Ashwini A Katre, Harrison Kim, Jinda Fan, Soldano Ferrone, Kurt R Zinn, Donald J Buchsbaum
INTRODUCTION: Novel therapies that effectively kill both differentiated cancer cells and cancer initiating cells (CICs), which are implicated in causing chemotherapy-resistance and disease recurrence, are needed to reduce the morbidity and mortality of ovarian cancer. These studies used monoclonal antibody (mAb) 376.96, which recognizes a B7-H3 epitope expressed on ovarian cancer cells and CICs, as a carrier molecule for targeted α-particle radioimmunotherapy (RIT) in preclinical models of human ovarian cancer...
January 10, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28104528/cannabinoid-receptor-type-2-cb2-as-one-of-the-candidate-genes-in-human-carotid-plaque-imaging-evalu1ation-of-the-novel-radiotracer-11-c-rs-016-targeting-cb2-in-atherosclerosis
#9
Romana Meletta, Roger Slavik, Linjing Mu, Zoran Rancic, Nicole Borel, Roger Schibli, Simon M Ametamey, Stefanie D Krämer, Adrienne Müller Herde
INTRODUCTION: Endarterectomized human atherosclerotic plaques are a valuable basis for gene expression studies to disclose novel imaging biomarkers and therapeutic targets, such as the cannabinoid receptor type 2 (CB2). In this work, CB2 is expressed on activated immune cells, which are abundant in inflamed plaques. We evaluated the CB2-specific radiotracer [(11)C]RS-016 for imaging vascular inflammation in human and mouse atherosclerotic lesions. METHODS: The differential gene expression of microscopically classified human carotid plaques was evaluated using quantitative polymerase chain reaction...
January 8, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28126682/a-multi-species-evaluation-of-the-radiation-dosimetry-of-11-c-erlotinib-the-radiolabeled-analog-of-a-clinically-utilized-tyrosine-kinase-inhibitor
#10
J Ryan Petrulli, Søren B Hansen, Galith Abourbeh, Maqsood Yaqub, Idris Bahce, Daniel Holden, Yiyun Huang, Nabeel B Nabulsi, Joseph N Contessa, Eyal Mishani, Adriaan A Lammertsma, Evan D Morris
INTRODUCTION: Erlotinib is a tyrosine kinase inhibitor prescribed for non-small cell lung cancer (NSCLC) patients bearing epidermal growth factor receptor mutations in the kinase domain. The objectives of this study were to (1) establish a human dosimetry profile of [(11)C]erlotinib and (2) assess the consistency of calculated equivalent dose across species using the same dosimetry model. METHODS: Subjects examined in this multi-species study included: a stage IIIa NSCLC patient, 3 rhesus macaque monkeys, a landrace pig, and 4 athymic nude-Fox1nu mice...
January 2, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28110124/monoanionic-99m-tc-tricarbonyl-aminopolycarboxylate-complexes-with-uncharged-pendant-groups-radiosynthesis-and-evaluation-as-potential-renal-tubular-tracers
#11
Malgorzata Lipowska, Jeffrey Klenc, Nashwa Jarkas, Luigi G Marzilli, Andrew T Taylor
INTRODUCTION: (99m)Tc(CO)3-nitrilotriacetic acid, (99m)Tc(CO)3(NTA), is a new renal tubular agent with pharmacokinetic properties comparable to those of (131)I-OIH but the clearance of (99m)Tc(CO)3(NTA) and (131)I-OIH is still less than the clearance of PAH, the gold standard for the measurement of effective renal plasma flow. At physiological pH, dianionic (99m)Tc(CO)3(NTA) has a mononegative inner metal-coordination sphere and a mononegative uncoordinated carboxyl group. To evaluate alternate synthetic approaches, we assessed the importance of an uncoordinated carboxyl group, long considered essential for tubular transport, by evaluating the pharmacokinetics of three analogs with the (99m)Tc(CO)3(NTA) metal-coordination sphere but with uncharged pendant groups...
December 27, 2016: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28110123/investigation-of-123-i-production-using-electron-accelerator
#12
Albert Avetisyan, Robert Avagyan, Ruben Dallakyan, Gohar Avdalyan, Nikolay Dobrovolsky, Vasak Gavalyan, Ivetta Kerobyan, Gevorg Harutyunyan
The possibility of (123)I isotope production with the help of the high-intensity bremsstrahlung photons produced by the electron beam of the LUE50 linear electron accelerator at the A.I. Alikhanyan National Science Laboratory (Yerevan Physics Institute [YerPhI]) is considered. The production method has been established and shown to be successful. The (124)Xe(γ,n)(123)Xe→(123)I nuclear reaction has been investigated and the cross-section was calculated by nuclear codes TALYS 1.6 and EMPIRE 3.2. The optimum parameter of the thickness of the target was determined by GEANT4 code...
December 22, 2016: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28063322/quantitation-of-rat-cerebral-blood-flow-using-99m-tc-hmpao
#13
Chie Suzuki, Shintaro Kimura, Mutsumi Kosugi, Yasuhiro Magata
INTRODUCTION: Technetium-99m-hexamethylpropyleneamine oxime ((99m)Tc-HMPAO) is potentially useful for the assessment of cerebral blood flow (CBF) in small animals. In this paper, a procedure for quantitation of rat CBF using (99m)Tc-HMPAO was determined. METHODS: Biodistribution of (99m)Tc-radioactivity in normal rats was determined after intravenous administration of (99m)Tc-HMPAO. Acetazolamide treated rats were intravenously administered with the mixture of (99m)Tc-HMPAO and N-isopropyl-[(125)I]iodoamphetamine ([(125)I]IMP), and arterial blood was then collected for 5min...
December 22, 2016: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28043006/synthesis-and-evaluation-of-a-99m-tc-tricarbonyl-labeled-somatostatin-receptor-targeting-antagonist-peptide-for-imaging-of-neuroendocrine-tumors
#14
Lauren Radford, Fabio Gallazzi, Lisa Watkinson, Terry Carmack, Ashley Berendzen, Michael R Lewis, Silvia S Jurisson, Dionysia Papagiannopoulou, Heather M Hennkens
INTRODUCTION: A somatostatin receptor (SSTR)-targeting antagonist peptide (sst2-ANT) was radiolabeled with (99m)Tc tricarbonyl via a tridentate [N,S,N]-type ligand (L) to develop a radiodiagnostic agent, (99m)TcL-sst2-ANT, for imaging of SSTR-expressing neuroendocrine tumors. METHODS: Receptor affinity was assessed in vitro with the nonradioactive analogue, ReL-sst2-ANT, via a challenge experiment in AR42J cells with (125)I-SS-14 as the competing radioligand. Preparation of (99m)TcL-sst2-ANT was achieved via reaction of [(99m)Tc(CO)3(H2O)3](+) with L-sst2-ANT...
December 9, 2016: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28013122/development-of-11-c-3-h-thk-5351-a-potential-novel-carbon-11-tau-imaging-pet-radioligand
#15
Vladimir Stepanov, Marie Svedberg, Zhisheng Jia, Raisa Krasikova, Laetitia Lemoine, Nobujuki Okamura, Shozo Furumoto, Nicholas Mitsios, Jan Mulder, Bengt Långström, Agneta Nordberg, Christer Halldin
INTRODUCTION: Due to the rise in the number of patients with dementia the imperative for finding new diagnostic and treatment options becomes ever more pressing. While significant progress has been made in PET imaging of Aβ aggregates both in vitro and in vivo, options for imaging tau protein aggregates selectively are still limited. Based on the work previously published by researchers from the Tohoku University, Japan, that resulted in the development of [(18)F]THK-5351, we have undertaken an effort to develop a carbon-11 version of the identical structure - [(11)C]THK-5351...
December 9, 2016: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28012346/pet-studies-in-non-human-primates-choosing-drug-doses
#16
EDITORIAL
Michael R Kilbourn
No abstract text is available yet for this article.
December 9, 2016: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28013121/radiopharmaceutical-chemistry-of-targeted-radiotherapeutics-part-4-strategies-for-211-at-labeling-at-high-activities-and-radiation-doses-of-211-at-%C3%AE-particles
#17
Oscar R Pozzi, Michael R Zalutsky
INTRODUCTION: Alpha particles are radiation of high energy and short range, properties that can lead to radiolysis-mediated complications in labeling chemistry at the high radioactivity levels required for clinical application. In previous papers in this series, we have shown that radiation dose has a profound effect on the astatine species that are present in the labeling reaction and their suitability for the synthesis of N-succinimidyl 3-[(211)At]astatobenzoate. The purpose of this study was to evaluate the effects of adding N-chlorosuccinimide (NCS) to the methanol solution used for initial isolation of (211)At after distillation, a process referred to as (211)At stabilization, on (211)At chemistry after exposure to high radiation doses...
March 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28013120/intraarticular-and-intravenous-administration-of-99m-tc-hmpao-labeled-human-mesenchymal-stem-cells-99m-tc-ah-mscs-in-vivo-imaging-and-biodistribution
#18
Luis Meseguer-Olmo, Antonio Jesús Montellano, Teresa Martínez, Carlos M Martínez, Beatriz Revilla-Nuin, Marta Roldán, Cristina Fuente Mora, Maria Dolores López-Lucas, Teodomiro Fuente
INTRODUCTION: Therapeutic application of intravenous administered (IV) human bone marrow-derived mesenchymal stem cells (ahMSCs) appears to have as main drawback the massive retention of cells in the lung parenchyma, questioning the suitability of this via of administration. Intraarticular administration (IAR) could be considered as an alternative route for therapy in degenerative and traumatic joint lesions. Our work is outlined as a comparative study of biodistribution of (99m)Tc-ahMSCs after IV and IAR administration, via scintigraphic study in an animal model...
March 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/27915165/re-assessing-gallium-67-as-a-therapeutic-radionuclide
#19
Muhamad F Bin Othman, Nabil R Mitry, Valerie J Lewington, Philip J Blower, Samantha Y A Terry
INTRODUCTION: Despite its desirable half-life and low energy Auger electrons that travel further than for other radionuclides, (67)Ga has been neglected as a therapeutic radionuclide. Here, (67)Ga is compared with Auger electron emitter (111)In as a potential therapeutic radionuclide. METHODS: Plasmid pBR322 studies allowed direct comparison between (67)Ga and (111)In (1MBq) in causing DNA damage, including the effect of chelators (EDTA and DTPA) and the effects of a free radical scavenger (DMSO)...
March 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28034416/do-we-say-what-we-mean-and-mean-what-we-say-setting-the-record-straight-on-radiochemistry-nomenclature
#20
LETTER
Heinz H Coenen, Antony D Gee
No abstract text is available yet for this article.
February 2017: Nuclear Medicine and Biology
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