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Current Radiopharmaceuticals

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https://www.readbyqxmd.com/read/28294075/%C3%AE-18f-fluoro-azomycin-arabinoside-%C3%AE-18f-faza-synthesis-radiofluorination-and-preliminary-pet-imaging-of-murine-a431-tumors
#1
Piyush Kumar, Peter Roselt, Gerald Reischl, Carlene Cullinane, Davood Beiki, Walter Ehrlichmann, David Binns, Ebrahim Naimi, Jennifer Yang, Rodney Hicks, Hans-Juergen Machulla, Leonard I Wiebe
BACKGROUND: 1-α-D-(5-Deoxy-5-[18F]fluoroarabinofuranosyl)-2-nitroimidazole ([18F]FAZA) is a PET radiotracer that demonstrates excellent potential in imaging regional hypoxia, and is clinically used in diagnosing a wide range of solid tumors in cancer patients. [18F]FAZA, however, is radiofluorinated in only moderate recovered radiochemical yield (rRCY, ~12%). It is postulated that the relative stability of the C1' β-anomeric bond at C5' will make 1-β-D-(5-fluoro-5-deoxyarabinofuranosyl)-2-nitroimidazole (β-FAZA), the β-conformer of FAZA, an attractive candidate for clinical hypoxia imaging...
March 13, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28183248/new-horizons-on-molecular-pharmacology-applied-to-drug-discovery-when-resonance-overcomes-radioligand-binding
#2
Larissa Pernomian, Mayara Santos Gomes, Josimar Moreira Dornelas, Carlos Henrique Tomich de Paula da Silva, Jaoaquín María Campos Rosa, Cristina Ribeiro De Barros Cardoso
One of the cornerstones of rational drug development is the measurement of molecular parameters derived from ligand-receptor interaction, which guides therapeutic windows definition. Over the last decades, radioligand binding has provided valuable contributions in this field as key method for such purposes. However, its limitations spurred the development of more exquisite techniques for determining such parameters. For instance, safety risks related to radioactivity waste, expensive and controlled disposal of radioisotopes, radiotracer separation-dependence for affinity analysis, and one-site mathematical models-based fitting of data make radioligand binding a suboptimal approach in providing measures of actual affinity conformations from ligands and G protein-coupled receptors (GPCR)...
February 8, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28164753/evaluation-of-the-influence-of-the-conjugation-site-of-the-chelator-agent-hynic-to-glp1-antagonist-radiotracer-for-insulinoma-diagnosis
#3
Bluma Linkowski Faintuch, Daniele Seo, Érica Aparecida De Oliveira, Roselaine Campos Targino, Ana Maria Moro
Radiotracer diagnosis of insulinoma, can be done using somatostatin or glucagon-like peptide 1 (GLP-1). Performance of GLP-1 antagonists tends to be better than of agonists. We investigated the uptake of the antagonist exendin (9-39), radiolabeled with technetium-99m. Two different sites of the biomolecule were selected for chelator attachment. HYNIC-βAla chelator attached to serine (C- terminus) of exendin, was associated with higher tumor uptake than to aspartate (N- terminus). In conclusion the chelator position in the biomolecule influenced receptor uptake...
January 26, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28124595/a-sensitive-method-for-the-measurement-of-copper-at-trace-levels-using-an-hplc-based-assay
#4
Jason L J Dearling, Alan B Packard
BACKGROUND: Measurement of trace metal contamination is critical in the production of radiometals, such as 64Cu, for protein labeling. ICP-MS provides these data with high sensitivity and high specificity, but at high (instrument) cost. TETA (1,4,8,11-tetraazacyclotetradecane-1,4,8,11-tetraacetic acid) titration provides high sensitivity at low cost but with low specificity. A method that allowed the measurement of trace metals with high sensitivity but also at relatively low cost would, therefore, be very useful in the development of new radiometal production methods...
January 25, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28056732/development-of-a-radiolabeled-amlodipine-analog-for-l-type-calcium-channel-imaging
#5
Tahereh Firouzyar, Amir Reza Jalilian, Mohammad Reza Aboudzadeh, Hossein Sadeghpour, Mehrban Pooladi, Mahdi Shafiee-Ardestani, Ali Khalaj
PURPOSE: The non-invasive imaging and quantification of L-type calcium channels in living tissues is of great interest in diagnosis of congestive heart failure, myocardial hypertrophy, irritable bowel syndrome etc. METHODS: Technetium-<sup>99m</sup> labeled amlodipine conjugate ([<sup>99m</sup>Tc]-DTPA-AMLO) was prepared starting freshly eluted (<1 h) <sup>99m</sup>Technetium pertechnetate (86.5 MBq) and conjugated DTPA-AMLO at pH 5 in 30 min at room temperature in high radiochemical purity (>99%, RTLC; specific activity: 55-60 GBq/mmol)...
January 4, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28034352/development-of-a-novel-carbon-11-labeled-pet-radioligand-for-melanin-concentrating-hormone-receptor-1
#6
Hideyuki Igawa, Vladimir Stepanov, Lenke Tari, Shoki Okuda, Syunsuke Yamamoto, Shizuo Kasai, Yasutaka Nagisa, Jenny Häggkvist, Marie Svedberg, Miklós Tóth, Akihiro Takano, Christer Halldin
Melanin-concentrating hormone (MCH) is an attractive target for antiobesity agents and many drug discovery programs have been dedicated to identify small-molecule antagonists of melanin-concentrating hormone receptor 1 (MCHR1). The aim of this study was to develop a positron emission tomography (PET) tracer for MCHR1 for translation of preclinical pharmacology to clinic to enhance success rate of drug discovery programs. We identified 4-(cyclopropylmethoxy)-N-[8-methyl-3-({[(1-methyl-1H-pyrrol-2-yl)methyl]amino}ethyl)quinolin-7-yl]benzamide (Compound II) from Takeda MCHR1 antagonist library by utilizing binding affinity, log D value, physicochemical parameters ideal for a central nerve system agent, and synthetic feasibility of corresponding carbon-11 labeled radioligands as selection parameters for tracer candidates...
December 30, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28034351/synthesis-and-preliminary-evaluation-of-5-18f-fluoroleucine
#7
Bennett B Chin, Darryl McDougald, Douglas Weitzel, Thomas Hawk, Robert E Reiman, Michael R Zalutsky, Ganesan Vaidyanathan
BACKGROUND: Amino acid transporters, such as LAT1, are overexpressed in aggressive prostate and breast carcinomas, directly influencing pathways of growth and proliferation. OBJECTIVE: The purpose of this study is to synthesize and characterize a novel 18F labeled leucine analog, 5-[18F]fluoroleucine, as a potential imaging agent for aggressive tumors which may not be amenable to imaging by FDG PET. METHODS: 5-fluoroleucine was synthesized and characterized, and its 18F-labeled analog was synthesized from a mesylate precursor...
December 30, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28034291/radiopharmaceuticals-for-diagnosis-and-therapy-of-neuroendocrine-differentiated-prostate-cancer
#8
Giampiero Giovacchini, Elisabetta Giovannini, Mattia Riondato, Andrea Ciarmiello
Neuroendocrine differentiation of prostate cancer (PCa) is a relatively frequent event, generally understudied, that carries important prognostic information. It is most frequently observed during the advanced stages of disease, when PCa has lost its sensitivity to androgen deprivation therapy or to chemotherapy, moderate to diffuse bone metastatic spread dominates the imaging scenario and it is responsible for painful clinical symptomatology. However, evidences indicate that neuroendocrine differentiation is a progressive phenomenon that starts at the very early part of the pathogenesis of cancer transformation contributing to it...
December 29, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/27855612/99mtc-labeled-white-blood-cell-scan-as-a-guide-to-open-biopsy-in-the-management-of-hip-and-knee-prosthesis-infection-preliminary-results
#9
Mauro Liberatore, Giuseppe Gentile, Giulia Anna Follacchio, Viviana Frantellizzi, Giuseppe De Vincentis, Francesco Monteleone, Christos Anagnostou, Francesco Maria Drudi, Vittorio Calvisi
The aim of the present prospective study was to evaluate the usefulness of labeled leukocyte scan as a guide to open biopsy for the management of hip and knee prosthesis infection in patients without loosening of orthopedic device. Twenty-six patients with suspected hip (24) and knee (2) prosthesis infection underwent routine analysis of blood, plain radiography and 99m Tc-HMPAO labelled leukocyte scan (WBCS). On these basis, patients were subdivided in the following groups: bone infection without loosening (n°=14), septic loosening (n°=8), superficial infection (n°=2), no infection (n°=2)...
November 17, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/27804868/gallium-68-in-medical-imaging
#10
Lucia Martiniova, Louis De Palatis, Elba Etchebehere, Gregory Ravizzini
Over the past several years, Positron Emission Tomography (PET) imaging agents labeled with 68Gallium (68Ga) have undergone a significant increase in clinical utilization. 68Ga is conveniently produced from a germanium-68/gallium-68 (68Ge/68Ga) generator. Because of the compact size and ease of use of the generator, 68Ga labeled compounds may be more cost-effective than PET radioisotopes that are cyclotron-produced. The convenient half-life of 68Ga (T1/2=68 min) provides sufficient radioactivity for various PET imaging applications, while delivering acceptable radiation doses to patients...
October 28, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/27774910/18f-fluoroestradiol-positron-emission-tomography-in-breast-cancer-patients-systematic-review-of-the-literature-meta-analysis
#11
Laura Evangelista, Maria Vittoria Dieci, Valentina Guarneri, Pier Franco Conte
PURPOSE: The aim of the study was to determine the correlation between 16α-18F-fluoro-17β-estradiol (18F-FES) uptake and the expression and functionality of estrogen receptors (ERs), as well as to evaluate the ability of 18F-FES PET to predict the response to hormonal therapy (HT) in patients with locally advanced or metastatic breast cancer (BC). METHODS: Literature searches in the major literature databases were carried out in order to select English-language articles dealing with 18F-FES PET and BC...
October 19, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/27748184/177lu-dota-bevacizumab-radioimmunotherapy-agent-for-melanoma
#12
Ximena Camacho, Victoria Calzada, Marcelo Fernández, Omar Alonso, Roger Chammas, Eloisa Riva, Juan Pablo Gambini, Pablo Cabral
BACKGROUND: Vascular endothelial growth factor (VEGF) is one of the classic factors to tumor-induced angiogenesis in several types, including melanoma. Bevacizumab is a humanized monoclonal antibody directed against VEGF. OBJECTIVE: To radiolabel Bevacizumab with 177-Lutetium as a potential radioimmunotherapy agent for melanoma. METHODS: Bevacizumab was derivatized with DOTA-NHS-ester at 4 ºC for 18 h. DOTA-Bevacizumab was radiolabeled with 177LuCl3 (15 MBq/mg) at 37 ºC for 1 h...
October 10, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/27527071/combination-treatment-of-glioblastoma-by-low-dose-radiation-and-genistein
#13
Vahid Changizi, Atefeh Zamanian, Hasan Nedaie, Saeed Amanpour, Mahnaz Haddadi
PURPOSE: Gioblastoma multiforme as a chemoresistant and radioresistant malignant cell line needs to novel strategies to treatment. Low-dose hyper-radiosensitivity (LDHRS) seems to be an effective phenomenon to irradiation that can save normal brain fibroblasts. Genistein which is a soy isoflavone can be cytotoxic in some tumor cell lines. So we determined to study the effect of combining these two treatment modalities. MATERIALS AND METHODS: After 30 hours incubation with Genistein in different concentrations on U87MG cell line, proliferation and clonogenicity were conducted by both clonogenic and MTT assays...
August 13, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/27562785/automated-pet-radiotracer-manufacture-on-the-bg75-system-imaging-validation-studies-of-18f-fluoromisonidazole-18f-fmiso
#14
Hong Yuan, Jonathan E Frank, Joseph R Merrill, Daniel A Hillesheim, Mark H Khachaturian, Atilio Anzellotti
The study aimed to develop the method of automated production on the hypoxia radiotracer 1-[18F]fluoro-3-(2-nitro-1H-imidazol-1-yl)-propan-2-ol ([18F]FMISO) on the novel fully automated platform of the BG75 system. Further validation of [18F]FMISO hypoxia imaging functionality in two tumor mouse models (FaDu/U87) was evaluated using PET/CT imaging, and the distribution of [18F]FMISO was validated by the standard hypoxia marker EF5. The average radiochemical purity was (99 ± 1) % and the average pH was 5.5 ± 0...
July 25, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/27363481/dual-nuclear-fluorescence-imaging-potantial-of-zinc-ii-phthalocyanine-in-mia-paca-2-cell-line
#15
Fatma Yurt Lambrecht, Mine Ince, Ozge Er, Kasim Ocakoglu, Cagla Kayabasi, Cumhur Gunduz, Fatma Aslıhan Sarı
Pancreatic cancer is very common and difficult to diagnose in early stage. Imaging systems for diagnosing cancer have many disadvantages. However, combining different imaging modalities offer synergistic advantages. Optical imaging is the most multidirectional and widely used imaging modality in both clinical practice and research. In present study, Zinc(II) phthalocyanine [Zn(II)Pc] was synthesized, labeled with iodine-131 and in vitro study was carried out. The intracellular uptake studies of radiolabeled Zn(II)Pc were performed in WI-38 [ATCC CCL-75™, tissue: human fibroblast lung] and MIA PaCa-2 [ATCC CRL-1420™, tissue: human epithelial pancreas carcinoma] cell lines...
June 27, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/27237136/radiosynthesis-of-18f-fluorobenzoate-doxorubicin-using-acylation-approach
#16
Pardeep Kumar, Ankit Watts, Pratap Acharya, Ranju Bansal, Anchal Ghai, Amritjyot Kaur, Baljinder Singh
This study describes the two steps method for radio synthesis of fluorine-18 [18F] labeled doxorubicin. A quaternary salt of the precursor pentamethylbenzyl-4-(trimethylammonium trifluoromethanesulfonate) benzoate was synthesized and characterized. As a first step, 4-[18F]-fluorobenzoic acid (FBA) was synthesized from precursor and used as an intermediate to label doxorubicin. In the second step, [18F]-FBA was attached to the primary amine of doxorubicin by acylation reaction. The total reaction time for the synthesis of [18F]-FBA-doxorubicin was about 60 minutes...
May 30, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/27210819/18f-fdg-pet-ct-in-patients-affected-by-differentiated-thyroid-carcinoma-with-positive-thyroglobulin-level-and-negative-131i-whole-body-scan-it-s-value-confirmed-by-a-bicentric-experience
#17
Francesco Bertagna, Domenico Albano, Giovanni Bosio, Arnoldo Piccardo, Bassam Dib, Raffaele Giubbini
BACKGROUND: 18F-FDG-PET/CT applications in the field of differentiated thyroid cancer (DTC) are continuously growing. OBJECTIVE: To retrospectively analyze in a wide population enrolled in two nuclear medicine centers the diagnostic value of 18F-FDG-PET/CT in patients treated with 131I and negative 131I-WBS but in presence of Tg levels higher than 1ng/ml after TSH stimulation. METHOD: From September 2005 to December 2014, 154 patients affected by DTC, treated with 131I with negative 131I-WBS and Tg≥1ng/ml underwent 18F-FDG-PET/CT...
May 23, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/27150277/production-of-68ga-citrate-based-on-a-sno2-generator-for-short-term-turpentine-oil-induced-inflammation-imaging-in-rats
#18
Alireza Mirzaei, Amir R Jalilian, Mehdi Akhlaghi, Davood Beiki
INTRODUCTION: Gallium-68 citrate has been successfully applied in the PET imaging of infections and inflammation in some centers; however further evaluation of the tracer in inflammation models is of great importance. METHODS: 68Ga-citrate prepared from [68Ga]GaCl3 (eluted form an SnO2 based 68Ge/68Ga generator) and sodium citrate at optimized conditions followed by quality control tests was injected to normal and turpentine-oil induced rats PET/CT imaging studies up to 290 min...
May 6, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/27593257/hypoxia-radiotracer-produced-automatically-in-dose-on-demand-fashion
#19
Hong Yuan, Jonathan E Frank, Joseph R Merrill, Daniel A Hillesheim, Mark H Khachaturian, Atilio I Anzellotti
No abstract text is available yet for this article.
2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/27593256/preliminary-experience-with-yttrium-90-labelled-rituximab-chimeric-anti-cd-20-antibody-in-patients-with-relapsed-and-refractory-b-cell-non-hodgkins-lymphoma
#20
Parul Thakral, Suhas Singla, Atul Vashist, Madhav P Yadav, Santosh K Gupta, Jaya S Tyagi, Atul Sharma, Chandra S Bal, EmptyYN Y Snehlata, Arun Malhotra
BACKGROUND AND OBJECTIVES: The aim of the study is to evaluate the therapeutic efficacy and safety of Yttrium- 90 radiolabelled chimeric anti CD20 antibody-Rituximab in the treatment of patients with relapsed/ refractory B cell Non-Hodgkins Lymphoma (NHL). METHODS: Twenty patients with relapsed/refractory CD20+ NHL in progressive state were included in the study. These patients had undergone a median of 2 (range 2-5) prior standard chemotherapy ± immunotherapy regimens...
2016: Current Radiopharmaceuticals
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