Design and synthesis of enantiopure 18 F-labelled [18 F]trifluoromethyltryptophan from 2-halotryptophan derivatives via copper(I)-mediated [18 F]trifluoromethylation and evaluation of its in vitro characterization for the serotonergic system imaging.

abstract：:Radiolabelling of cocaine-derived 3-phenyltropanes for dopamine transporter positron emission tomography with (18) F and (11) C is reviewed. ...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Riss PJ,Stockhofe K,Roesch F

更新日期：2013-03-01 00:00:00

abstract：:Enzymatic conversion of a drug can be an efficient alternative for the preparation of a complex metabolite compared with a multi-step chemical synthesis approach. Limitations exist for chemical methods for direct oxygen incorporation into organic molecules often suffering from low yields and unspecific oxidation and a...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Poraj-Kobielska M,Atzrodt J,Holla W,Sandvoss M,Gröbe G,Scheibner K,Hofrichter M

更新日期：2013-07-01 00:00:00

abstract：:MMP-9 is a zinc-dependent endopeptidase that is involved in the proteolytic degradation of the extracellular matrix and plays an important role in cancer migration, invasion, and metastasis. The aim of this study was to evaluate the potential of MMP-tracers [18 F]BR420 and [18 F]BR351 for MMP-9 imaging in a colorectal...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Vazquez N,Missault S,Vangestel C,Deleye S,Thomae D,Van der Veken P,Augustyns K,Staelens S,Dedeurwaerdere S,Wyffels L

更新日期：2017-01-01 00:00:00

abstract：:The Maillard reaction of sugars and amines resulting in the formation of glycosylamines and Amadori products is of biological significance, for drug delivery, role in central nervous system, and other potential applications. We have examined the interaction of (18) F-fluorodeoxyglucose ((18) F-FDG) with biological ami...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Baranwal A,Patel HH,Mukherjee J

更新日期：2014-02-01 00:00:00

abstract：:A novel phosphonium salt bearing a fluorine-18 labelled triazole has been designed as a potential imaging agent for apoptosis. The radiosynthesis of [1-(2-[(18)F]fluoroethyl),1H[1,2,3]triazole 4-ethylene] triphenylphosphonium bromide ([(18)F]MitoPhos_01) has been carried out on a fully automated system in a two-step r...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Haslop A,Gee A,Plisson C,Long N

更新日期：2013-05-30 00:00:00

abstract：:Withdrawal: Jianfeng Liu et al. 'The radiosynthesis of novel PI3K inhibitor, 8-ethoxy-2-(4-[18 F]fluorophenyl)-3-nitro-2H-chromene (18 F-EFPNC)', Journal of Labelled Compounds and Radiopharmaceuticals (https://doi.org/10.1002/jlcr.3524). The above article, published online on 30 May 2017 on Wiley Online Library (wiley...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Liu J,Sun J,Li Y,Su P,Hou G,Han J

更新日期：2020-12-01 00:00:00

abstract：:Alzheimer's disease (AD) and related dementias show increasing clinical prevalence, yet our understanding of the etiology and pathobiology of disease-related neurodegeneration remains limited. In this regard, noninvasive imaging with radiotracers for positron emission tomography (PET) presents a unique tool for quanti...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Holland JP,Liang SH,Rotstein BH,Collier TL,Stephenson NA,Greguric I,Vasdev N

更新日期：2014-04-01 00:00:00

abstract：:Metabolism, environmental fate, and low concentration food residue studies would be facilitated by the use of radiolabeled test articles that can be readily quantified within complex matrices. However, radiochemical approaches for such studies require high specific activities to allow analytical detection of correspon...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Singh A,Hakk H,Lupton SJ

更新日期：2018-04-01 00:00:00

abstract：:A series of (13)C-labeled polyaromatic hydrocarbons (PAHs), fluorenols and phenanthrenols were synthesized from commercially available (13)C-labeled starting material giving rise to M + 6 isotopomers. This was accomplished using key palladium-catalyzed cross-coupling and one-carbon homologation strategies. The conditi...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Wu R,Silks LA,Olivault-Shiflett M,Williams RF,Ortiz EG,Stotter P,Kimball DB,Martinez RA

更新日期：2013-09-01 00:00:00

abstract：:[15 N]-Cholamine is an isotope tag for metabolomics research, because it possesses 2 important properties: an NMR active isotope and a permanent charge for MS sensitivity. Here, we present a scalable synthesis of [15 N]-cholamine. ...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Szeto J,Lemoine R,Nguyen R,Olson LL,Tanga MJ

更新日期：2018-04-01 00:00:00

abstract：:The development of bacteria-specific infection radiotracers is of considerable interest to improve diagnostic accuracy and enabling therapy monitoring. The aim of this study was to determine if the previously reported radiolabelled 1,4,7,10-tetraazacyclododecane-N,N',N″,N‴-tetraacetic acid (DOTA) conjugated peptide [6...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Nielsen KM,Jørgensen NP,Kyneb MH,Borghammer P,Meyer RL,Thomsen TR,Bender D,Jensen SB,Nielsen OL,Alstrup AKO

更新日期：2018-05-23 00:00:00

abstract：:The increasing application of positron emission tomography and single-photon emission computer tomography in radiopharmacy and nuclear medicine has stimulated the development of a multitude of novel and versatile bioorthogonal conjugation techniques. Currently, there is particular interest in radiolabeling biologicall...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Mamat C,Gott M,Steinbach J

更新日期：2018-03-01 00:00:00

abstract：:The labeling of peptides with gallium-68 is often initially performed by manual labeling, but with high clinical demand, other alternatives are needed. Cold-kits or automated synthesis are viable options for standardized methods and deemed pharmaceutically more acceptable. This study compares these [68 Ga]Ga-PSMA-11 p...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Kleynhans J,Rubow S,le Roux J,Marjanovic-Painter B,Zeevaart JR,Ebenhan T

更新日期：2020-11-01 00:00:00

abstract：:In this study, we developed a saccharin (SAC)-based radiopharmaceutical (68 Ga-NOTA-SAC) and evaluated the possibility of its application as a PET tracer in the diagnosis of carbonic anhydrase IX (CA IX)-overexpressed tumors. We did a water-soluble tetrazolium assay and flow cytometry analysis to identify the cell via...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Shin UC,Choi JS,Beak YJ,Lee MW,Kim HS,Choi DW,Kim DG,Kim SW

更新日期：2020-10-29 00:00:00

abstract：:3-Amino-4-(1,1-difluoro-propyl)-6-(4-methanesulfonyl-piperidin-1-yl)-thieno[2,3-b]pyridine-2-carboxylic acid amide (1) is a potent IκB Kinase-β (IKK-β) inhibitor. The efficient preparations of this compound labeled with carbon-14 and deuterium are described. The carbon-14 synthesis was accomplished in six radiochemica...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Latli B,Eriksson M,Hrapchak M,Busacca CA,Senanayake CH

更新日期：2016-06-30 00:00:00

abstract：:Hydroxyzine and aripiprazole are active pharmaceutical ingredients that have been largely acknowledged for their antipsychotic properties. Deuterium labeled isotopes of hydroxyzine and aripiprazole are internal standards that can aid in the further research of non-isotopic forms via quantification analysis using HPLC-...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Vohra M,Sandbhor M,Wozniak A

更新日期：2015-06-15 00:00:00

abstract：:Labeling agents with radioisotopes or fluorescent dyes are useful for investigating the biodistributions of biologically active proteins and peptides. Compared with molecular imaging with a single modality, dual imaging probes provide complementary information for each modality. The development of a dual radioisotope/...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Watanabe H,Itagaki F,Shimizu Y,Iikuni S,Ono M

更新日期：2019-11-01 00:00:00

abstract：:A simple and rapid nonradioactive iodide labeling/radiolabeling method for peptides, using an inexpensive oxidizing agent such as sodium hypochlorite and a cyclic peptide, cRGDyK (cyclo Arg-Gly-Asp-d-Tyr-Lys), was developed in this work. Labeling reaction was optimized by conducting experiments under variable ratios o...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Doll S,Woolum K,Kumar K

更新日期：2016-09-01 00:00:00

abstract：:Dimethylsulfoniopropionate (DMSP, (2-carboxyethyl)dimethylsulfonium) is a highly abundant compound in marine environments. As a precursor to the climatically active gas, dimethylsulfide (DMS), DMSP connects the marine and terrestrial sulfur cycles. However, the fate of DMSP in microbial biomass is not well understood ...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Wirth JS,Whitman WB

更新日期：2019-01-01 00:00:00

abstract：:Flavin nucleotides, i.e. flavin mononucleotide (FMN) and flavin adenine dinucleotide (FAD), are utilized as prosthetic groups and/or substrates by a myriad of proteins, ranging from metabolic enzymes to light receptors. Isotopically labeled flavins have served as invaluable tools in probing the structure and function ...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Mishanina TV,Kohen A

更新日期：2015-07-01 00:00:00

abstract：:Asparagine-glycine-arginine (NGR)-containing peptides targeting aminopeptidase N (APN)/CD13 can be an excellent candidate for targeting ligands in molecular tumor imaging. In this study, we developed two NGR-containing hexapeptides, and evaluated the diagnostic performance of Tc-99m labeled hexapeptides as molecular i...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Kim DW,Kim WH,Kim MH,Kim CG

更新日期：2015-02-01 00:00:00

abstract：:Aporphines are attractive candidates for imaging D2 receptor function because, as agonists rather than antagonists, they are selective for the receptor in the high affinity state. In contrast, D2 antagonists do not distinguish between the high and low affinity states, and in vitro data suggests that this distinction m...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Sromek AW,Zhang S,Akurathi V,Packard AB,Li W,Alagille D,Morley TJ,Baldwin R,Tamagnan G,Neumeyer JL

更新日期：2014-12-01 00:00:00

abstract：:We describe the dramatic differences in the synthesis and physiological and pharmacokinetical profiling of two sodium-glucose cotransporter (SGLT) drug candidates AVE2268 and AVE8887 with very similar chemical structures. It is a classic example of how a radioactive study was able to spare resources in preclinical dev...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Schudok M,Glombik H,Derdau V

更新日期：2020-07-07 00:00:00

abstract：:18 F-radiolabeled diphenyl gallium thiosemicarbazone was prepared by [18 F] fluoride exchange of a nitrato anion under mild conditions. The diphenyl gallium thiosemicarbazone chloride is easily prepared in gram quantities and can be used at room temperature in the presence of oxygen. The corresponding nitrate complex ...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Venkatachalam TK,Stimson DHR,Bhalla R,Mardon K,Bernhardt PV,Reutens DC

更新日期：2019-06-15 00:00:00

abstract：:A robust medium-scale (approximately 3 g) synthetic method for 15 N labeling of pyridine (15 N-Py) is reported based on the Zincke reaction. 15 N enrichment in excess of 81% was achieved with approximately 33% yield. 15 N-Py serves as a standard substrate in a wide range of studies employing a hyperpolarization techni...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Chukanov NV,Kidd BE,Kovtunova LM,Bukhtiyarov VI,Shchepin RV,Chekmenev EY,Goodson BM,Kovtunov KV,Koptyug IV

更新日期：2019-11-01 00:00:00

abstract：:In this paper, we disclose a new strategy for the radiosynthesis of [18 F]PARPi from the corresponding, boc-protected, nitro-precursor. Using a two-step procedure, [18 F]PARPi could be isolated in radiochemical yields up to 9.6%. The reaction proceeds via an efficient one-pot, two-step process, allowing for simplifica...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Wilson TC,Pillarsetty N,Reiner T

更新日期：2020-07-01 00:00:00

abstract：:The nucleosides zidovudine (AZT), stavudine (d4T), and telbivudine (LdT) are approved for use in the treatment of human immunodeficiency virus (HIV) and hepatitis B virus (HBV) infections. To promote positron emission tomography (PET) imaging studies on their pharmacokinetics, pharmacodynamics, and applications in can...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Zhang Z,Doi H,Koyama H,Watanabe Y,Suzuki M

更新日期：2014-06-30 00:00:00

abstract：:Bone pain is the major manifestation of skeletal metastases. Although various treatment modalities are available for bone pain palliation, use of radiolabeled phosphonates is documented to be more effective. Among radionuclides available for this purpose, lutetium-177 is gaining popularity due to its moderate beta ene...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Kumar C,Sharma R,Das T,Korde A,Sarma H,Banerjee S,Dash A

更新日期：2018-09-01 00:00:00

abstract：:With the recent ability to use combined liquid chromatography/electrospray tandem mass spectrometry to analyze for several eicosanoids in biological samples in a single and rapid experiment, heavy isotope-labeled eicosanoids are needed as internal standards in order to quantify eicosanoid analytes. The present study d...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Ghomashchi F,Bollinger JG,Gelb MH

更新日期：2007-07-17 00:00:00

abstract：:A decline of norepinephrine transporter (NET) level is associated with several psychiatric and neurological disorders. Therefore positron emission tomography (PET) imaging agents are greatly desired to study the NET pathway. We have developed a C-fluoropropyl analog of nisoxetine: (R)-N-methyl-3-(3'-[(18)F]fluoropropy...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Nguyen VL,Pichika R,Bhakta PH,Kant R,Mukherjee J

更新日期：2010-02-09 00:00:00