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Nuclear Medicine and Biology

Weiyan Zhou, Weiqi Bao, Donglang Jiang, Yanyan Kong, Fengchun Hua, Xiuhong Lu, Yihui Guan
INTRODUCTION: The objective of this study was to synthesize an N-methyl-d-aspartate receptor (NMDAR) radiotracer [18 F]-GE-179 in one-pot and evaluate its in vivo binding for NMDAR activation after brain ischemia reperfusion injury. METHODS: [18 F]-GE-179 was auto-synthesized using a quick one-pot method from a stable disulfide precursor and purified using semi-preparative high-performance liquid chromatography (HPLC) with ethanol/aqueous NaH2 PO4 as the eluent...
April 25, 2018: Nuclear Medicine and Biology
Benjamin B Kasten, Abhishek Gangrade, Harrison Kim, Jinda Fan, Soldano Ferrone, Cristina R Ferrone, Kurt R Zinn, Donald J Buchsbaum
No abstract text is available yet for this article.
April 25, 2018: Nuclear Medicine and Biology
Ksenia Lisova, Maxim Sergeev, Susan Evans-Axelsson, Andreea D Stuparu, Seval Beykan, Jeffrey Collins, Jason Jones, Michael Lassmann, Ken Herrmann, David Perrin, Jason T Lee, Roger Slavik, R Michael van Dam
BACKGROUND: Peptides labeled with positron-emitting isotopes are emerging as a versatile class of compounds for the development of highly specific, targeted imaging agents for diagnostic imaging via positron-emission tomography (PET) and for precision medicine via theranostic applications. Despite the success of peptides labeled with gallium-68 (for imaging) or lutetium-177 (for therapy) in the clinical management of patients with neuroendocrine tumors or prostate cancer, there are significant advantages of using fluorine-18 for imaging...
April 20, 2018: Nuclear Medicine and Biology
Kazuma Ogawa, Ryohei Masuda, Yoshiaki Mizuno, Akira Makino, Takashi Kozaka, Yoji Kitamura, Yasushi Kiyono, Kazuhiro Shiba, Akira Odani
INTRODUCTION: Sigma-1 receptor is a target for tumor imaging. In a previous study, we synthesized a vesamicol analog, (+)-2-[4-(4-bromophenyl)piperidino]cyclohexanol [(+)-pBrV], with a high affinity for sigma-1 receptor, and synthesized radiobrominated (+)-pBrV. This radiobrominated (+)-pBrV showed high tumor uptake in tumor-bearing mice; however, radioactivity accumulation in normal tissues, such as the liver, was high. We assumed that the accumulation of (+)-pBrV in the non-target tissues was partially derived from its high lipophilicity; therefore, we synthesized and evaluated (+)-4-[1-(2-hydroxycyclohexyl)piperidine-4-yl]-2-bromophenol [(+)-BrV-OH], which is a more hydrophilic compound...
April 6, 2018: Nuclear Medicine and Biology
Ali Ouadi, Virgile Bekaert, Nicolas Receveur, Lionel Thomas, François Lanza, Patrice Marchand, Christian Gachet, Pierre H Mangin, David Brasse, Patrice Laquerriere
INTRODUCTION: Platelets play a major role in thrombo-embolic diseases, notably by forming a thrombus that can ultimately occlude a vessel. This may provoke ischemic pathologies such as myocardial infarction, stroke or peripheral artery diseases, which represent the major causes of death worldwide. The aim of this study was to evaluate the specificity of radiolabeled Rat-Anti-Mouse antibody (RAM.1). METHODS: We describe a method to detect platelets by using a RAM...
March 17, 2018: Nuclear Medicine and Biology
Áron Roxin, Chengcheng Zhang, Sungjoon Huh, Mathieu L Lepage, Zhengxing Zhang, Kuo-Shyan Lin, François Bénard, David M Perrin
INTRODUCTION: The transmembrane α4 β1 integrin receptor, or very-late antigen 4 (VLA-4), is associated with tumor metastasis and angiogenesis, the development of chemotherapeutic drug resistance, and is overexpressed in multiple myelomas, osteosarcomas, lymphomas, leukemias, and melanomas. The peptidomimetic, LLP2A, is a high-affinity ligand with specificity for the extracellular portion of VLA-4 and several conjugates have been evaluated in vivo by NIR-fluorescence,111 In-SPECT and68 Ga- and64 Cu-PET imaging, but to date, not with18 F-PET...
March 12, 2018: Nuclear Medicine and Biology
Tilman Läppchen, Yvonne Kiefer, Jason P Holland, Mark D Bartholomä
INTRODUCTION: We recently developed a chelating platform based on the macrocycle 1,4,7-triazacyclononane with up to three five-membered azaheterocyclic arms for complexation of the PET nuclides gallium-68 and copper-64. The main objective of this study was to evaluate the stability and pharmacokinetics of68 Ga- and64 Cu-complexes of the bifunctional chelator NODIA-Me 1 covalently bound to a PSMA targeting vector in vivo. METHODS: NODIA-Me 1 was conjugated to the PSMA targeting Glu-NH-CO-NH-Lys moiety to give the bioconjugate NODIA-Me-NaI-Ahx-PSMA 4...
March 10, 2018: Nuclear Medicine and Biology
Yutian Feng, Anthony J DeGraffenreid, Michael D Phipps, Tammy L Rold, Nkemakonam C Okoye, Fabio A Gallazzi, Charles L Barnes, Cathy S Cutler, Alan R Ketring, Timothy J Hoffman, Silvia S Jurisson
INTRODUCTION: Trithiol chelates are suitable for labeling radioarsenic (72 As: 2.49 MeV β+ , 26 h;77 As: 0.683 MeV β- , 38.8 h) to form potential theranostic radiopharmaceuticals for PET imaging and therapy. To investigate the in vivo stability of trithiol chelates complexed with no carrier added (nca) radioarsenic, a bifunctional trithiol chelate was developed, and conjugated to bombesin(7-14)NH2 as a model peptide. METHODS: A trithiol-BBN(7-14)NH2 bioconjugate and its arsenic complex were synthesized and characterized...
March 10, 2018: Nuclear Medicine and Biology
L Fiedler, M Kellner, A Gosewisch, R Oos, G Böning, S Lindner, N Albert, P Bartenstein, H-J Reulen, R Zeidler, F J Gildehaus
INTRODUCTION: Due to their infiltrative growth behavior, gliomas have, even after surgical resection, a high recurrence tendency. The approach of intracavitary radioimmunotherapy (RIT) is aimed at inhibiting tumor re-growth by directly administering drugs into the resection cavity (RC). Direct application of the radioconjugate into the RC has the advantage of bypassing the blood-brain barrier, which allows the administration of higher radiation doses than systemic application. Carbonic anhydrase XII (CA XII) is highly expressed on glioma cells while being absent from normal brain and thus an attractive target molecule for RIT...
March 4, 2018: Nuclear Medicine and Biology
J D Andersson, B Thomas, S V Selivanova, E Berthelette, J S Wilson, A J B McEwan, K Gagnon
This paper presents the irradiation and processing of high-current100 Mo targets at the University of Alberta (UofA) in a GMP compliant setting. For purpose of comparison with a second production facility, additional studies at Centre Hospitalier Universitaire de Sherbrooke (CHUS) are also described. INTRODUCTION: More than 70% of today's diagnostic radiopharmaceuticals are based on99m Tc, however the conventional supply chain for obtaining99m Tc is fragile. The aim of this work was to demonstrate reliable high yield production and processing of99m Tc with medium-energy, high-current, cyclotrons...
March 2, 2018: Nuclear Medicine and Biology
Tomoyuki Ohya, Kotaro Nagatsu, Hisashi Suzuki, Masami Fukada, Katsuyuki Minegishi, Masayuki Hanyu, Ming-Rong Zhang
INTRODUCTION: Copper-67 is an attractive beta emitter for targeted radionuclide therapy. However, the availability of 67 Cu limits its potential use in a wide range of applications. In this study, we propose an easy small-scale production of 67 Cu using 64 Ni target for a preclinical study. METHODS: 67 Cu was produced from an electrodeposited 64 Ni target via the 64 Ni(α, p)67 Cu-reaction with a 36 MeV alpha beam at 15 eμA (electrical microampere) conducted for 7 h...
April 2018: Nuclear Medicine and Biology
Duo Xu, Rongqiang Zhuang, Linyi You, Zhide Guo, Xiangyu Wang, Chenyu Peng, Deliang Zhang, Pu Zhang, Hua Wu, Weimin Pan, Xianzhong Zhang
INTRODUCTION: A novel radiotracer 1‑(2‑(2‑(2‑[18 F]fluoroethoxy)ethoxy)ethyl)‑1H‑1,2,3‑triazole‑estradiol ([18 F]FETE) was successfully synthesized, characterized and evaluated in mice for estrogen receptor (ER)-positive breast cancer targeting with positron emission tomography (PET) imaging. METHODS: The tosylate precursor 3 was radiolabeled with 18 F and then reacted with 17α‑ethinyl‑estradiol to produce the final [18 F]FETE. The physicochemical properties of [18 F]FETE were tested in vitro, including determination of the octanol/water partition coefficient, stability and cellular uptake in MCF-7 (ER-positive) and MDA-MB-231 (ER-negative) cells...
April 2018: Nuclear Medicine and Biology
Zhihao Zha, Karl Ploessl, Seok Rye Choi, Zehui Wu, Lin Zhu, Hank F Kung
INTRODUCTION: Prostate specific membrane antigen (PSMA) is a well-established target for diagnostic and therapeutic applications for prostate cancer. It is know that [68 Ga]PSMA 11 ([68 Ga]Glu-NH-CO-NH-Lys(Ahx)-HBED-CC) is the most well studied PET imaging agent for detecting over expressed PSMA binding sites of tumors in humans. In an effort to provide new agents with improved characteristics for PET imaging, we report a novel [68 Ga]-Glu-NH-CO-NH-Lys(Ahx)-linker-HBED-CC conjugate with a novel O-(carboxymethyl)-L-tyrosine, as the linker group...
April 2018: Nuclear Medicine and Biology
Jothilingam Sivapackiam, Richard Laforest, Vijay Sharma
INTRODUCTION: 68 Ga[Ga]-Galmydar is an avid transport substrate of ABCB1 (P-Glycoprotein; 170kDa plasma membrane protein), breast cancer resistance protein (BCRP; ABCG2; 72kDa), penetrates human epidermal carcinoma (KB3-1), breast cancer (MCF7), embryonic kidney (HEK 293) tumor cells and rat cardiomyoblasts, and localizes within the mitochondria of tumor and myocardium cells. 68 Ga[Ga]-Galmydar excretes from blood pool quickly, and shows stable retention within rat myocardium in vivo for extended periods, therefore, the agent shows potential to enable myocardial perfusion imaging...
April 2018: Nuclear Medicine and Biology
Nariman Nezami, Nima Kokabi, Juan C Camacho, David M Schuster, Minzhi Xing, Hyun S Kim
INTRODUCTION: There are two different types of 90 Y Microspheres, glass and resin, in the market for 90 Y radioembolization (90 Y-RE). This study aimed to investigate the dose of radiation delivered through glass vs. resin-based 90 Y-RE to intrahepatic cholangiocarcinoma (ICC). METHODS: In this retrospective study, 10 patients with ICC underwent 90 Y-RE, five underwent glass (Glass group) and other 5 resin (Resin group) microspheres. Technetium-99m macro-aggregated albumin (Tc-99m MAA) shunt study was performed two weeks before 90 Y-RE...
April 2018: Nuclear Medicine and Biology
Hailey A Houson, Gregory N Nkepang, Andria F Hedrick, Vibhudutta Awasthi
Positron emission tomography (PET) of myocardial infarction (MI) by infarct avid imaging has the potential to reduce the time to diagnosis and improve diagnostic accuracy. The objective of this work was to synthesize 18 F-labeled glucaric acid (FGA) for PET imaging of isoproterenol-induced cardiomyopathy in a rat model. METHODS: We synthesized 18 F-FGA by controlled oxidation of 18 F-fluorodeoxy glucose (FDG), mediated by 4-acetamido-2,2,6,6-tetramethylpiperidine 1-oxyl (TEMPO) in presence of NaBr and NaOCl in highly-buffered reaction conditions...
April 2018: Nuclear Medicine and Biology
Wen Jing Zhu, Masato Kobayashi, Kohei Yamada, Kodai Nishi, Kotaro Takahashi, Asuka Mizutani, Ryuichi Nishii, Leo G Flores, Naoto Shikano, Munetaka Kunishima, Keiichi Kawai
INTRODUCTION: Due to its poor prognosis, specific imaging for early detection of malignant melanoma is strongly desired. Although radioiodine labeled 4-hydroxyphenylcysteamine, which we previously developed, has good affinity for tyrosinase, an enzyme in the melanin metabolic pathway, image contrast of the melanoma:organ ratios is not sufficiently high for detection of primary melanoma and metastases at early injection times. In this study, we developed radioiodine labeled acetaminophen (I-AP) for specific, high-contrast imaging of malignant melanoma...
April 2018: Nuclear Medicine and Biology
Anne-Sophie Salabert, Erick Mora-Ramirez, Marie Beaurain, Mathieu Alonso, Charlotte Fontan, Hafid Belhadj Tahar, Marie Laure Boizeau, Mathieu Tafani, Manuel Bardiès, Pierre Payoux
INTRODUCTION: The aim of this work was to study the biodistribution, metabolism and radiation dosimetry of rats injected with [18 F]FNM using PET/CT images. This novel radiotracer targeting NMDA receptor has potential for investigation for neurological and psychiatric diseases. METHODS: Free fraction and stability in fresh human plasma were determined in vitro. PET/CT was performed on anesthetized rats. Organs were identified and 3D volumes of interest (VOIs) were manually drawn on the CT in the center of each organ...
April 2018: Nuclear Medicine and Biology
Benjamin B Kasten, Abhishek Gangrade, Harrison Kim, Jinda Fan, Soldano Ferrone, Cristina R Ferrone, Kurt R Zinn, Donald J Buchsbaum
INTRODUCTION: We recently validated monoclonal antibody (mAb) 376.96 as an effective carrier for targeted α-particle radioimmunotherapy (RIT) with 212 Pb in ovarian cancer mouse models. In this study, we tested the binding of radiolabeled mAb 376.96 to human pancreatic ductal adenocarcinoma (PDAC) cells and localization in xenografts in immune-deficient mice and evaluated 212 Pb-labeled 376.96 (212 Pb-376.96) for PDAC therapy. METHODS: In vitro Scatchard assays assessed the specific binding of 212 Pb-376...
March 2018: Nuclear Medicine and Biology
Karolin Wagener, Dorothea Moderegger, Mareli Allmeroth, Achim Reibel, Stefan Kramer, Barbara Biesalski, Nicole Bausbacher, Rudolf Zentel, Oliver Thews, Frank Rösch
BACKGROUND: For the evaluation of macromolecular drug delivery systems suitable pre-clinical monitoring of potential nanocarrier systems is needed. In this regard, both short-term as well as long-term in vivo tracking is crucial to understand structure-property relationships of polymer carrier systems and their resulting pharmacokinetic profile. Based on former studies revealing favorable in vivo characteristics for 18 F-labeled random (ran) copolymers consisting of N-(2-hydroxypropyl)methacrylamide (HPMA) and lauryl methacrylate (LMA) - including prolonged plasma half-life as well as enhanced tumor accumulation - the presented work focuses on their long-term investigation in the living organism...
March 2018: Nuclear Medicine and Biology
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