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Nuclear Medicine and Biology

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https://www.readbyqxmd.com/read/29154145/evaluation-of-a-novel-grpr-antagonist-for-prostate-cancer-pet-imaging-64-cu-dotha2-peg-rm26
#1
Nematallah Mansour, Michel Paquette, Samia Ait-Mohand, Véronique Dumulon-Perreault, Brigitte Guérin
INTRODUCTION: Gastrin releasing peptide receptors (GRPRs) are significantly over-expressed on a large proportion of prostate cancers making them prime candidates for receptor-mediated nuclear imaging by PET. Recently, we synthesized a novel bifunctional chelator (BFC) bearing hydroxamic acid arms (DOTHA2). Here we investigated the potential of a novel DOTHA2-conjugated, (64)Cu-radiolabeled GRPR peptide antagonist, [D-Phe(6)-Sta(13)-Leu(14)-NH2]bombesin(6-14) (DOTHA2-PEG-RM26) to visualize prostate tumors by PET imaging...
October 23, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29117904/the-past-present-and-the-promise-of-the-future-of-nuclear-medicine-and-biology
#2
EDITORIAL
W C Eckelman, A D Windhorst, C O'Hara
No abstract text is available yet for this article.
October 12, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29055836/assessment-of-psma-targeting-ligands-bearing-novel-chelates-with-application-to-theranostics-stability-and-complexation-kinetics-of-68-ga-3-111-in-3-177-lu-3-and-225-ac-3
#3
James M Kelly, Alejandro Amor-Coarasa, Anastasia Nikolopoulou, Dohyun Kim, Clarence Williams, Shankar Vallabhajosula, John W Babich
INTRODUCTION: Recent successes in the treatment of metastatic castration-resistant prostate cancer (mCRPCa) by systemic endoradiotherapy has sparked renewed interest in developing small molecule ligands targeting prostate-specific membrane antigen (PSMA) and chelators capable of stable complexation of metal radionuclides for imaging and therapy. As the size and coordination number of metals for imaging, such as (68)Ga(3+), and for targeted therapy, such as (177)Lu(3+) and (225)Ac(3+), are substantially different, they may show a preference for macrocycles of different denticity...
October 3, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29074076/consensus-nomenclature-rules-for-radiopharmaceutical-chemistry-setting-the-record-straight
#4
REVIEW
Heinz H Coenen, Antony D Gee, Michael Adam, Gunnar Antoni, Cathy S Cutler, Yasuhisa Fujibayashi, Jae Min Jeong, Robert H Mach, Thomas L Mindt, Victor W Pike, Albert D Windhorst
Over recent years, within the community of radiopharmaceutical sciences, there has been an increased incidence of incorrect usage of established scientific terms and conventions, and even the emergence of 'self-invented' terms. In order to address these concerns, an international Working Group on 'Nomenclature in Radiopharmaceutical Chemistry and related areas' was established in 2015 to achieve clarification of terms and to generate consensus on the utilisation of a standardised nomenclature pertinent to the field...
October 2, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29031230/astatine-211-labeled-anti-her2-5f7-single-domain-antibody-fragment-conjugates-radiolabeling-and-preliminary-evaluation
#5
Jaeyeon Choi, Ganesan Vaidyanathan, Eftychia Koumarianou, Choong Mo Kang, Michael R Zalutsky
INTRODUCTION: Derived from heavy chain only camelid antibodies, ~15-kDa single-domain antibody fragments (sdAbs) are an attractive platform for developing molecularly specific imaging probes and targeted radiotherapeutics. The rapid tumor accumulation and normal tissue clearance of sdAbs might be ideal for use with (211)At, a 7.2-h half-life α-emitter, if appropriate labeling chemistry can be devised to trap (211)At in cancer cells after sdAb binding. This study evaluated two reagents, [(211)At]SAGMB and iso-[(211)At]SAGMB, for this purpose...
September 19, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29125999/preclinical-evaluation-of-heat-denatured-18-f-fdg-labeled-red-blood-cells-for-detecting-splenic-tissues-with-pet-in-rats
#6
Yohji Matsusaka, Tadaki Nakahara, Kazuhiro Takahashi, Yu Iwabuchi, Yuji Ogata, Chiyoko Nishime, Mayumi Kajimura, Masahiro Jinzaki
INTRODUCTION: Heat-denatured (99m)Tc-labeled red blood cells (RBCs) are used for detecting splenic tissues with scintigraphy. The present study aimed to evaluate the feasibility of using heat-denatured [(18)F]fluorodeoxyglucose ([(18)F]FDG)-labeled RBCs in detecting splenic tissues using positron emission tomography (PET) in rats. METHODS: RBCs were washed with phosphate buffered saline, labeled with [(18)F]FDG at 38°C, and heat-denatured at 50°C for 15 min. In vitro stability was assessed by measuring extracellular radioactivity during the 0-180 min incubation at 37°C...
September 18, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29031229/-99m-tc-duramycin-for-cell-death-imaging-impact-of-kit-formulation-purification-and-species-difference
#7
Luca Palmieri, Filipe Elvas, Christel Vangestel, Koon Pak, Brian Gray, Sigrid Stroobants, Steven Staelens, Leonie Wyffels
INTRODUCTION: [(99m)Tc]duramycin is a SPECT tracer for cell death imaging. We evaluated the impact of kit formulation, purification and species difference on the pharmacokinetic profile and cell death targeting properties of [(99m)Tc]duramycin in order to define the optimal conditions for (pre-)clinical use. METHODS: Three kits were prepared (A: traditional formulation, B: containing 1/3 of ingredients, C: containing HYNIC-PEG12-duramycin). Following labeling, the kits were used without purification, or with SPE or HPLC purification...
September 14, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29028502/dota-tetrazine-probes-with-modified-linkers-for-tumor-pretargeting
#8
Tilman Läppchen, Raffaella Rossin, Tiemen R van Mourik, Guillaume Gruntz, Freek J M Hoeben, Ron M Versteegen, Henk M Janssen, Johan Lub, Marc S Robillard
INTRODUCTION: Pretargeted radioimmunoimaging and -therapy approaches building on the bioorthogonal inverse-electron-demand Diels-Alder (IEDDA) reaction between strained trans-cyclooctenes (TCO) and electron-deficient tetrazines (Tz) have yielded impressive results in recent years and have proven a vital alternative to biological pretargeting systems. After improvement of the TCO-antibody conjugates, we here report on our evaluation of a new series of radiolabeled Tz-probes. METHODS: Four new Tz-probes were synthesized, radiolabeled with lutetium-177, and characterized in vitro in terms of lipophilicity, reactivity, and stability in PBS and mouse serum...
September 14, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29031997/a-six-year-longitudinal-pet-study-of-11-c-dtbz-binding-to-the-vmat2-in-monkey-brain
#9
Michael R Kilbourn, Robert A Koeppe
INTRODUCTION: The longitudinal reproducibility of in vivo binding potential measures for [(11)C]dihydrotetrabenazine ([(11)C]DTBZ) binding to the vesicular monoamine transporter 2 (VMAT2) site in primate brain was examined using a unique dataset of repeated control PET imaging studies. METHODS: Forty-one dynamic [(11)C]DTBZ PET studies were completed in a single rhesus monkey. Imaging equipment (microPET P4), personnel, radiotracer characteristics (injected mass amounts, molar activity) and image data analysis (BPND-Logan) were consistent throughout the entire sequence of PET studies...
September 5, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29031113/cross-sectional-and-longitudinal-small-animal-pet-shows-pre-and-post-synaptic-striatal-dopaminergic-deficits-in-an-animal-model-of-hiv
#10
Sanhita Sinharay, Dianne Lee, Swati Shah, Siva Muthusamy, Georgios Z Papadakis, Xiang Zhang, Dragan Maric, William C Reid, Dima A Hammoud
INTRODUCTION: In vivo imaging biomarkers of various HIV neuropathologies, including dopaminergic dysfunction, are still lacking. Towards developing dopaminergic biomarkers of brain involvement in HIV, we assessed the pre and postsynaptic components of the dopaminergic system in the HIV-1 transgenic rat (Tg), a well-characterized model of treated HIV+ patients, using small-animal PET imaging. METHODS: Fifteen to 18 month-old Tg and wild type (WT) rats were imaged with both [18F]-FP-CMT, a dopamine transporter (DAT) ligand (n=16), and [18F]-Fallypride, a D2/D3 dopamine receptor (D2/D3DR) ligand (n=16)...
August 31, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29100560/reconsider-logp
#11
LETTER
Chrysoula Vraka, Markus Mitterhauser
No abstract text is available yet for this article.
November 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29100559/is-logp-truly-dead
#12
LETTER
Michael R Kilbourn, Peter J H Scott
No abstract text is available yet for this article.
November 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28797928/comparison-of-planar-pet-and-well-counter-measurements-of-total-tumor-radioactivity-in-a-mouse-xenograft-model
#13
Michael V Green, Jurgen Seidel, Mark R Williams, Karen J Wong, Anita Ton, Falguni Basuli, Peter L Choyke, Elaine M Jagoda
INTRODUCTION: Quantitative small animal radionuclide imaging studies are often carried out with the intention of estimating the total radioactivity content of various tissues such as the radioactivity content of mouse xenograft tumors exposed to putative diagnostic or therapeutic agents. We show that for at least one specific application, positron projection imaging (PPI) and PET yield comparable estimates of absolute total tumor activity and that both of these estimates are highly correlated with direct well-counting of these same tumors...
October 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28692851/a-simple-device-to-convert-a-small-animal-pet-scanner-into-a-multi-sample-tissue-and-injection-syringe-counter
#14
Michael V Green, Jurgen Seidel, Peter L Choyke, Elaine M Jagoda
INTRODUCTION: We describe a simple fixture that can be added to the imaging bed of a small-animal PET scanner that allows for automated counting of multiple organ or tissue samples from mouse-sized animals and counting of injection syringes prior to administration of the radiotracer. The combination of imaging and counting capabilities in the same machine offers advantages in certain experimental settings. METHODS: A polyethylene block of plastic, sculpted to mate with the animal imaging bed of a small-animal PET scanner, is machined to receive twelve 5-ml containers, each capable of holding an entire organ from a mouse-sized animal...
October 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28648984/whole-body-biodistribution-of-the-cannabinoid-type-1-receptor-ligand-18-f-mk-9470-in-the-rat
#15
H G Buchholz, K Uebbing, S Maus, S Pektor, N Afahaene, V Weyer-Elberich, B Lutz, M Schreckenberger, I Miederer
The endocannabinoid system participates in many processes in the body, including memory, reward, pain, motor activity, food intake, energy metabolism, and gastrointestinal functions. [(18)F]MK-9470 is a positron emission tomography (PET) ligand that binds with high affinity and selectivity to the cannabinoid type 1 receptor. In order to fully characterize ligand behavior, tracer uptake measured using in vivo microPET was compared with results from ex vivo tissue dissection. Twelve male Sprague-Dawley rats were divided into three subgroups and scanned over time periods of 10min, 30min and 90min using PET...
September 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28636973/amide-to-triazole-switch-vs-in-vivo-nep-inhibition-approaches-to-promote-radiopeptide-targeting-of-grpr-positive-tumors
#16
Theodosia Maina, Aikaterini Kaloudi, Ibai E Valverde, Thomas L Mindt, Berthold A Nock
INTRODUCTION: Radiolabeled bombesin (BBN)-analogs have been proposed for diagnosis and therapy of gastrin-releasing peptide receptor (GRPR)-expressing tumors, such as prostate, breast and lung cancer. Metabolic stability represents a crucial factor for the success of this approach by ensuring sufficient delivery of circulating radioligand to tumor sites. The amide-to-triazole switch on the backbone of DOTA-PEG4-[Nle(14)]BBN(7-14) (1) was reported to improve the in vitro stability of resulting (177)Lu-radioligands...
September 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28628775/developing-new-pet-tracers-to-image-the-growth-hormone-secretagogue-receptor-1a-ghs-r1a
#17
Kazunori Kawamura, Masayuki Fujinaga, Yoko Shimoda, Tomoteru Yamasaki, Yiding Zhang, Akiko Hatori, Lin Xie, Hidekatsu Wakizaka, Katsushi Kumata, Takayuki Ohkubo, Yusuke Kurihara, Masanao Ogawa, Nobuki Nengaki, Ming-Rong Zhang
INTRODUCTION: `The growth hormone secretagogue receptor 1a (GHS-R1a) is the orphan G-protein-coupled receptor, and its endogenous ligand is ghrelin. GHS-R1a contributes to regulation of glucose homeostasis, memory and learning, food addiction, and neuroprotection. Several PET tracers for GHS-R1a have been developed, but none have been reported to be clinically applicable to GHS-R1a imaging. In this study, we developed three new PET tracers for GHS-R1a: (18)F-labeled 6-(4-chlorophenyl)-3-((1-(2-fluoroethyl)piperidin-3-yl)methyl)-2-(o-tolyl)quinazolin-4(3H)-one (1), (11)C-labeled 6-(4-chlorophenyl)-3-((1-(2-methoxyethyl)piperidin-3-yl)methyl)-2-(o-tolyl)quinazolin-4(3H)-one (2), and (11)C-labeled (S)-(4-(1H-indole-6-carbonyl)-3-methylpiperazin-1-yl)(4'-methoxy-[1,1'-biphenyl]-4-yl)methanone (3)...
September 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28624669/neutron-activatable-radionuclide-cancer-therapy-using-graphene-oxide-nanoplatelets
#18
Junghyun Kim, Michael Jay
Neutron-activation is a promising method of generating radiotherapeutics with minimal handling of radioactive materials. Graphene oxide nanoplatelets (GONs) were examined as a carrier for neutron-activatable holmium with the purpose of exploiting inherent characteristics for theranostic application. GONs were hypothesized to be an ideal candidate for this application owing to their desirable characteristics such as a rigid structure, high metal loading capacity, low density, heat resistance, and the ability to withstand harsh environments associated with the neutron-activation process...
September 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28602965/-67-ga-labeled-deferoxamine-derivatives-for-imaging-bacterial-infection-preparation-and-screening-of-functionalized-siderophore-complexes
#19
Joseph A Ioppolo, Deanna Caldwell, Omid Beiraghi, Lisset Llano, Megan Blacker, John F Valliant, Paul J Berti
INTRODUCTION: Deferoxamine (DFO) is a siderophore that bacteria use to scavenge iron and could serve as a targeting vector to image bacterial infection where current techniques have critical limitations. [(67)Ga]-DFO, which is a mimetic of the corresponding iron complex, is taken up by bacteria in culture, however in vivo it clears too rapidly to allow for imaging of infection. In response, we developed several new DFO derivatives to identify those that accumulate in bacteria, and at sites of infection, and that could potentially have improved pharmacokinetics...
September 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28599133/dose-on-demand-production-of-diverse-18-f-radiotracers-for-preclinical-applications-using-a-continuous-flow-microfluidic-system
#20
Lidia Matesic, Annukka Kallinen, Ivan Greguric, Giancarlo Pascali
INTRODUCTION: The production of (18)F-radiotracers using continuous flow microfluidics is under-utilized due to perceived equipment limitations. We describe the dose-on-demand principle, whereby the back-to-back production of multiple, diverse (18)F-radiotracers can be prepared on the same day, on the same microfluidic system using the same batch of [(18)F]fluoride, the same microreactor, the same HPLC column and SPE cartridge to obtain a useful production yield. METHODS: [(18)F]MEL050, [(18)F]Fallypride and [(18)F]PBR111 were radiolabeled with [(18)F]fluoride using the Advion NanoTek Microfluidic Synthesis System...
September 2017: Nuclear Medicine and Biology
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