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Journal of Labelled Compounds & Radiopharmaceuticals

Andrew V Mossine, Allen F Brooks, Vadim Bernard-Gauthier, Justin J Bailey, Naoko Ichiishi, Ralf Schirrmacher, Melanie S Sanford, Peter J H Scott
In this paper we describe the use of Cu-mediated [(18) F]fluorodeboronation for the automated production of PET radiotracers suitable for clinical use. Two recurrent issues with the method, low radiochemical conversion (RCC) on automation and protoarene byproduct purification issues, have been successfully addressed. The new method was utilized to produce sterile injectable doses of [(18) F]-(±)-IPMICF17, a PET radiotracer for tropomyosin receptor kinase B/C, using an automated synthesis module. Product was isolated in 1...
November 16, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Johannes Notni, Hans-Jürgen Wester
The potential and future role of certain metal radionuclides, for example, (44) Sc, (89) Zr, (86) Y, (64) Cu, (68) Ga, (177) Lu, (225) Ac, (213) Bi, and several terbium isotopes has been controversely discussed in the past decades. Furthermore, the possible benefits of "matched pairs" of isotopes for tandem applications of diagnostics and therapeutics (theranostics) have been emphasized, while such approaches still haven't made their way into routine clinical practice. Analysis of bibliographical data illustrates how popularity of certain nuclides has been promoted by cycles of availability and applications...
November 16, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Mohammad B Haskali, Peter D Roselt, Rodney J Hicks, Craig A Hutton
Radiolabelled peptides are vital tools used in positron emission tomography (PET) imaging for the diagnosis of disease, drug discovery and biomedical research. Peptides are typically labelled through conjugation to a radiolabelled prosthetic group, which usually necessitates complex, multi-step procedures, especially for fluorine-18 labelled peptides. Herein, we describe the automated synthesis and formulation of 2-[(18) F]fluoropropionate labelled RGD-peptides through use of the iPHASE Flexlab as an effective dual-stage radiochemical synthesis module...
November 16, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Mark M Goodman, Weiping Yu, Nashwa Jarkas
Fluorine-18 and iodine-123 labeled non-natural alicyclic and methyl branched disubstituted α,α-amino acids are a diverse and useful class of tumor imaging agents suitable for positron emission tomography (PET) and single photon emission computed tomography (SPECT). These tracers target the increased expression of the cell membrane amino acid transporter systems L, ASC and A exhibited by many human tumor cells. The most established clinical use for these radiolabeled amino acids is imaging primary and recurrent gliomas, and primary, recurrent and metastatic prostate cancer...
November 16, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Xiaoqing Zhuang, Dan Zhao, Pengfei Yang, Yingqin Jia, Rui Liang, Qian Zhao, Chunlei Han, Joseph M Kinsella, Ruilong Sheng, Juan Li
To analyze erythropoietin receptor (EpoR) status in tumors, recombinant human erythropoietin (rHuEpo) was labeled with (99m) Tc by (99m) Tc-centered one-pot synthesis, resulting in high radiochemical purity, stability and biological activity. Both in vitro cell culture experiments and biodistribution studies of normal rats demonstrated successful EpoR targeting. The biodistribution of labeled rHuEpo in a NCI-H1975 xenograft model showed tumor accumulation (tumor-to-muscle ratio: 4.27±1.77), confirming the expression of active EpoR in tumors...
November 15, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Judith A Egan, Crist N Filer
The two step synthesis of [(14) C]sodium ferrocyanide decahydrate is described. Ferrous hydroxide was prepared from iron powder and then reacted with [(14) C]sodium cyanide to afford the product. The [(14) C]sodium ferrocyanide decahydrate was characterized by HPLC and (13) C NMR.
November 15, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Kusum Vats, Drishty Satpati, Rohit Sharma, Chandan Kumar, Haladhar Dev Sarma, Sharmila Banerjee
The tripeptide sequence NGR (asparagine-glycine-arginine) specifically recognizes aminopeptidase N (APN or CD13) receptors highly expressed on tumor cells as well as tumor vasculature. Thus NGR peptides can precisely deliver therapeutic and diagnostic compounds to CD13 expressing cancer sites. In this regard two NGR peptide ligands, HYNIC-c(NGR) and HYNIC-PEG2 -c(NGR) were synthesized, radiolabeled with (99m) Tc and evaluated in CD13-positive human fibrosarcoma HT-1080 tumor xenografts. The radiotracers, (99m) Tc-HYNIC-c(NGR) and (99m) Tc-HYNIC-PEG2 -c(NGR) could be prepared in ~95% radiochemical purity (RCP) and exhibited excellent in vitro and in vivo stability...
November 15, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Simone Maschauer, Olaf Prante
The neurotensin receptors are overexpressed in various tumor types, especially in highly progressive pancreatic tumors. As this cancer has a poor 5-year survival prognosis, there is an urgent need to improve early diagnosis and treatment strategies. This review article provides an overview of the latest developments in radiopharmaceuticals for neurotensin receptor-positive tumors, including peptidic and non-peptidic radiopharmaceuticals, not only for SPECT and PET but also for endoradiotherapy.
November 7, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Francesco Spinelli, Linjing Mu, Simon M Ametamey
The cannabinoid type 2 (CB2) receptor is an immunomodulatory receptor mainly expressed in peripheral cells and organs of the immune system. The expression level of CB2 in the central nervous system under physiological conditions is negligible, however under neuroinflammatory conditions an upregulation of CB2 protein or mRNA mainly co-localized with activated microglial cells has been reported. Consequently, CB2 agonists have been confirmed to play a role in neuroprotective and anti-inflammatory processes. A suitable PET radioligand for imaging CB2 would provide an invaluable research tool to explore the role of CB2 receptor expression in inflammatory disorders...
November 6, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Syed M Qaim, Ingo Spahn
Medical radionuclide production technology is well established. There is, however, a constant need for further development of radionuclides. The present efforts are mainly devoted to non-standard positron emitters (e.g. (64) Cu, (86) Y, (124) I, (73) Se) and novel therapeutic radionuclides emitting low-range β(-) particles (e. g. (67) Cu, (186) Re), conversion or Auger electrons (e.g. (117m) Sn, (77) Br) and α-particles (e.g. (225) Ac). A brief account of various aspects of development work (i.e. nuclear data, targetry, chemical processing, quality control) is given...
November 6, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Lili Liang, Xueqian Zhang, Xiaoyu Su, Jianchun Li, Yong Tian, Hongbao Xue, Huiqin Xu
One type of biocompatible nanoparticles functionalized with folate and (99m) Tc, was successfully synthesized. Maleimide-folic acid (Mal-FA) was selected to covalently conjugate with -SH of the nanoparticles (NPs) to prepare NPs-FA for targeting. (99m) Tc was selected to conjugate with -NH2 and -SH groups of cysteine residues on the surface of nanoparticles to prepare NPs-FA-(99m) Tc for radioactive counting. The ability to target folate receptors of NPs-FA-(99m) Tc was assessed in uptake studies with folate-receptor-positive human HepG2 cells...
October 30, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Geerd-J Meyer
This educational review describes and summarizes the historic discovery of element 85, the experiments leading to its physical and chemical characterization and comparison with is lighter homologue iodine. The halflives of its longest living isotopes (210) At and (211) At with 8.3 h and 7.22 h respectively together with their alpha decay characteristics made these isotopes interesting for radiation biological research. However, the lack of stable isotopes of astatine presents a strong challenge for all characterizations...
October 28, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Alexander J Leeder, Lynda J Brown, Johanna Becker-Baldus, Michaela Mehler, Clemens Glaubitz, Richard C D Brown
Three all-trans retinals containing multiple (13) C labels have been synthesised to enable DNP enhanced solid-state MAS NMR studies of novel microbial retinylidene membrane proteins including proteorhodpsin and channelrhodopsin. The synthetic aproaches allowed specific introduction of (13) C labels in ring substituents and at different positions in the polyene chain to probe structural features such as ring orientation and interaction of the chromophore with the protein in the ground state and in photointermediates...
October 28, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Jianjun Wang, Wenjiang Yang, Jinquan Xue, Yanhua Zhang, Yu Liu
Melphalan (MFL) is a typical nitrogen mustard for the treatment of many types of cancer. For the purpose to develop novel (99m) Tc-labeled tumor imaging agents with SPECT, MFL was directly labeled by (99m) Tc using DTPA (diethylene triamine pentacetate acid) as bifunctional chelating agent. The novel ligands were successfully synthesized by conjugation of DTPA to melphalan to get mono-substituted DTPA-MFL and bis-substituted DTPA-2MFL. Radiolabeling was performed in high yield to get (99m) Tc-DTPA-MFL and (99m) Tc-DTPA-2MFL respectively, which were hydrophilic and stable at room temperature...
October 11, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Myoung Hyoun Kim, Chang Guhn Kim, Seul-Gi Kim, Dae-Weung Kim
We developed a Tc-99m and fluorescence labeled peptide, Tc-99m TAMRA-GHEG-ECG-VAPG to target tumor cells, and evaluated the diagnostic performance as a dual-modality imaging agent for tumor in a murine model. TAMRA-GHEG-ECG-VAPG was synthesized using Fmoc solid-phase peptide synthesis. Radiolabeling of TAMRA-GHEG-ECG-VAPG with Tc-99m was done using ligand exchange via tartrate. Binding affinity and in vitro cellular uptake studies were performed. Gamma camera imaging, biodistribution and ex vivo imaging studies were performed in murine models with SW620 tumors...
October 11, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Johannes Ermert
The increasing importance of the positron emission tomography (PET) in clinical diagnosis led to the development of a multitude of radiotracers labelled with positron emitting radionuclides of group 15 (pnicogens) and 16 (chalcogens) of the periodic table of elements. The positron emitters of the endogenous occurring elements nitrogen, phosphorus, oxygen and sulphur are characterized by very short half-lives compared to the most commonly used PET-radionuclides carbon-11 or fluorine-18. Therefore, the potential of their synthesis and possible applications in PET is challenging and limited...
October 11, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Duncan C Ellinwood, Mohamed F El-Mansy, Layhna S Plagmann, Jan F Stevens, Claudia S Maier, Adrian F Gombart, Paul R Blakemore
Xanthohumol [(E)-6´-methoxy-3´-(3-methylbuten-2-yl)-2´,4´,4´´-trihydroxychalcone], the principal prenylated flavonoid from hops, has a complex bioactivity profile and (13) C-labelled isotopomers of this compound are of potential use as molecular probes and as analytical standards to study metabolism and mode-of-action. 1,3-[(13) C]2 -Xanthohumol was prepared by an adaptation of the total synthesis of Khupse and Erhardt in 7 steps and 5.7% overall yield from phloroglucinol by a route incorporating a cascade Claisen-Cope rearrangement to install the 3´-prenyl moiety from a 5´-prenyl aryl ether and an aldol condensation between 1-[(13) C]-2´,4´-bis(benzyloxymethyloxy)-6´-methoxy-3´-(3-methylbuten-2-yl)acetophenone and 1´-[(13) C]-4-(methoxymethyloxy)benzaldehyde...
October 6, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Victor W Pike
Over the last two decades or so, hypervalent iodine compounds, such as diaryliodonium salts and aryliodonium ylides, have emerged as useful precursors for labeling homoarenes and heteroarenes with no-carrier-added cyclotron-produced [(18) F]fluoride ion (t1/2 = 109.8 min). They permit rapid and effective radiofluorination at electron-rich as well as electron-deficient aryl rings, and often with unrestricted choice of ring position. Consequently, hypervalent aryliodine compounds have found special utility as precursors to various small-molecule (18) F-labeling synthons and to many radiotracers for biomedical imaging with positron emission tomography...
October 5, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Mehdi Boudjemeline, Robert Hopewell, Pierre-Luc Rochon, Dean Jolly, Iness Hammami, Sylvia Villeneuve, Alexey Kostikov
Pittsburgh compound B ([(11) C]PiB) is the gold standard PET tracer for the in vivo imaging of amyloid plaques. Currently it is synthesized by either solution chemistry or using a "dry loop" approach followed by HPLC purification within 30 minutes starting from [(11) C]CO2 . Here we report a novel, highly efficient solid phase supported carbon-11 radiolabeling procedure using commercially available disposable tC18 cartridge as a "3-in-1" entity: reactor, purifier and solvent replacement system. [(11) C]PiB is synthesized by passing gaseous [(11) C]CH3 OTf through a tC18 cartridge preloaded with a solution of precursor...
October 5, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Joseph Downey, Salvatore Bongarzonev, Stefan Hader, Antony D Gee
Cyclotron-produced carbon-11 is a highly valuable radionuclide for the production of positron emission tomography (PET) radiotracers. It is typically produced as relatively unreactive carbon-11 carbon dioxide ([(11) C]CO2 ) which is most commonly converted into a more reactive precursor for synthesis of PET radiotracers. The development of [(11) C]CO2 fixation methods have more recently enabled the direct radiolabeling of a diverse array of structures directly from [(11) C]CO2 , and the advantages afforded by the use of a loop-based system employed in (11) C-methylation and (11) C-carboxylation reactions inspired us to apply the [(11) C]CO2 fixation "in-loop"...
October 4, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
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