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Current Radiopharmaceuticals

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https://www.readbyqxmd.com/read/28721805/automated-one-pot-radiosynthesis-of-11c-s-adenosyl-methionine
#1
Florencia Zoppolo, Williams Porcal, Patricia Oliver, Eduardo Osvaldo Savio, Henry Engler
BACKGROUND: Glycine-N-methyl transferase is an enzyme overexpressed in some neoplastic tissues. It catalyses the methylation of glycine using S-adenosyl methionine (SAM) as co-enzyme. SAM is involved in a great variety of biochemical processes, including transmethylation reactions. Thus, [11C]SAM could be used to evaluate transmethylation activity in tumours. The only method reported for [11C]SAM synthesis is an enzymatic process with several limitations. We propose a new chemical method to obtain [11C]SAM, through a one-pot synthesis...
July 18, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28714401/chemical-consequences-of-radioactive-decay-and-their-biological-implications
#2
Onofre T DeJesus
The chemical effects of radioactive decay arise from (1) transmutation, (2) formation of charged daughter nuclei, (3) recoil of the daughter nuclei, (4) electron "shakeoff" phenomenon and (5) vacancy cascade in decays via electron capture and internal conversion. This review aims to reiterate what has been known for a long time regarding the chemical consequences of radioactive decay and gives a historical perspective to the observations that led to their elucidation. The energetics of the recoil process in each decay mode is discussed in relation to the chemical bond between the decaying nucleus and the parent molecule...
July 14, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28681701/radiochemical-evaluation-and-in-vitro-assessment-of-the-targeting-ability-of-a-novel-99mtc-hynic-rgd-for-u87mg-human-brain-cancer-cells
#3
Hanieh Karimi, Nourollah Sadeghzadeh, Saeid Abediankenari, Farzaneh Rezazadeh, Fereshteh Hallajian
BACKGROUND: Labeled RGD peptide that specifically targets ανβ3 integrin has great potential for the early diagnosis of malignant tumors. αvβ3 integrin receptors appear specifically more on the surface of glioblastoma (malignant glioma) cells rather than normal cells. OBJECTIVE: The aim of this study was to identify a novel RGD that can be radiolabeled with 99mTc with in vitro assessment of its targeting ability for U87MG human brain cancer cells. METHOD: Novel RGD was designed by Amino Acid retro-inversion technique...
July 6, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28675994/effect-of-treatment-with-caspofungin-on-the-diagnosis-of-fungal-infections-by-gamma-scintigraphy
#4
L Fernández, A L Reyes, P Oliver, M Terán
The aim of this work is to assess the influence of treatment with unlabeled-Caspofungin, on the quality of diagnostic scintigraphic images of induced lesions in nude mice undergoing both bacterial and fungal infections and to determine the level of specificity of 99mTc-tricarbonyl-Caspofungin to discriminate between fungal or bacterial infections. In vitro studies on the behaviour of the 99mTc-tricarbonyl-Caspofungin complex binding percentage at different yeast concentrations of Candida albicans or Staphylococcus aureus were made...
July 3, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28637403/experiences-with-99mtc-hmpao-in-a-diagnostic-pathway-for-violent-patients-with-schizophrenic-spectrum-disorders
#5
Morten Jacobsen, Arvid Jensen, Guttorm Breivik Storvestre, Tone Marie Bergstrom, Diyar Nori Mohamad Rashi, Nielssen Bjorn, Wiktor Pal, Hymer Knut-Erik
Background and objective In a security ward we assessed the diagnostic contribution of single photon scintigraphy [SPECT] in our diagnostic pathway for patients with serious mental disease and a history of violence. Methods Twenty patients were examined between 2012 and 2015 and the findings compared to those in nine patients with the same diagnosis, but no history of violence. Results All violent patients had areas with reduced accumulation of 99mTc-HMPAO frontally and in the temporal lobe, in the non-violent group only two patients demonstrated these findings...
June 21, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28530534/biological-evaluation-of-99mtc-hynic-edda-tricine-ser-3-d4-peptide-for-tumor-targeting
#6
Ziba Kazemi, Mona Haddad Zahmatkesh, Seyed Mohammad Abedi, Seyed Jalal Hosseinimehr
BACKGROUND: D4 small peptide (Leu-Ala-Arg-Leu-Leu-Thr) was selected as an appropriate agent for specific targeting of epidermal growth factor receptor (EGFR). OBJECTIVE: The aim of study was to investigate the 99mTc-labeled D4 peptide for non small cell lung tumor targeting. METHOD: HYNIC-(Ser)3-D4 peptide was labeled with 99mTc using mixture of tricine and ethylenediamine diacetic acid (EDDA) as co-ligands. The in vitro cellular uptake of radiolabebled peptide was evaluated by blocking test on human non small lung cancer (A-549) cell line and its biodistribution was evaluated in A-549 xenografted nude mice...
May 19, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28530533/respiratory-motion-management-in-pet-ct-applications-and-clinical-usefulness
#7
Luca Guerra, Elena De Ponti, Sabrina Morzenti, Chiara Spadavecchia, Cinzia Crivellaro
Although breathing movement can introduce heavy bias in both image quality and quantitation, currently there is lack of interest for the respiratory motion management in PET/CT imaging. The respiratory gating technology has shown significant benefits on image quality, reducing motion related artifacts and increasing quantification. Indeed, many papers have demonstrated that there is a consistent increase of the Standardized Uptake Value (SUV) in gated PET images when compared to ungated ones, particularly for the small lesions located both in liver and in lung...
May 19, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28462719/intraoperative-localisation-of-impalpable-breast-lesions-utilising-the-rollis-technique-following-peritumoral-99mtc-colloid-sentinel-node-lymphoscintigraphy
#8
Te-Jui Hung, John Burrage, Anita Bourke, Donna Taylor
BACKGROUND: Ultrasound or stereotactic guided hook-wire localisation has been the standard-of-care for the pre-surgical localisation of impalpable breast lesions, which account for approximately a third of all breast cancer. Radioguided occult lesion localisation using I-125 seeds (ROLLIS) is a relatively new technique for guiding surgical excision of impalpable breast lesions, and is a promising alternative to the traditional hook-wire method. When combined with Tc-99m labelled colloid for sentinel node mapping in clinically indicated cases, there has been uncertainty regarding whether the downscatter of Tc-99m into the I-125 energy spectrum could adversely affect the intra-operative detection of the I-125 seed, especially pertaining to a peritumoral injection...
April 27, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28412923/fdg-pet-ct-predicts-outcome-in-oropharingeal-carcinoma-patients-undergoing-intensity-modulated-radiation-therapy-with-dose-escalation-to-fdg-avid-tumour-volumes
#9
Paola Mapelli, Sara Broggi, Elena Incerti, Pierpaolo Alongi, Margarita Kirienko, Claudio Fiorino, Italo Dell Oca, Federico Fallanca, Emilia Giovanna Vanoli, Nadia Gisella Di Muzio, Luigi Gianolli, Maria Picchio
PURPOSE: To evaluate the predictive value of FDG-PET/CT parameters on outcome of oropharyngeal squamocellular cancer (OSCC) patients undergoing helical tomotherapy (HTT), with dose escalation to FDG-PET/CT positive tumour volumes using the simultaneous integrated boost (SIB) technique. MATERIALS AND METHODS: We analysed 41 patients studied by FDG-PET/CT and treated with radical intent between 2005 and 2014 for OSCC. HTT-SIB was delivered in 30 fractions concomitantly: 69 Gy, as SIB, to the PET-positive volume (biological target volume - BTV-PET), both to the primary tumour (T) and lymph nodes (N), 66 Gy to the T and positive N, 54 Gy to the laterocervical nodes at risk...
April 13, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28332450/nuclear-medicine-in-patients-with-net-radiolabeled-somatostatin-analogues-and-their-brothers
#10
Vincenzo Cuccurullo, Maria Rosaria Prisco, Giuseppe Danilo Di Stasio, Luigi Mansi
Although Somastostatin (SS) scintigraphy (SRS) has been introduced many years ago, it remains the most diffuse radionuclide diagnostic tool in patients with neuroendocrine tumours (NETs). Being SS receptors (SSTR) expressed in the majority of NETs, radiolabeled SS analogues (SS-A) provide high diagnostic accuracy, mainly in patients with gastro-entero-pancreatic (GEP) tumors. SSTR are the best target for radiotracers used either for diagnostic and therapeutic purposes in NETs due to their presence on the surface of neoplastic cells of clinical interest...
March 23, 2017: Current Radiopharmaceuticals
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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/27748184/177lu-dota-bevacizumab-radioimmunotherapy-agent-for-melanoma
#20
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
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