Synthesis of stable isotope-labeled nasturlexins and potential precursors to probe biosynthetic pathways of cruciferous phytoalexins.

abstract：:Palladium(II)-mediated oxidative carbonylation reactions have been used to synthesize (11) C-radiolabelled ureas via the coupling of amines with [(11) C]carbon monoxide, in a one-pot process. Following trapping of (11) CO in a solution of copper(I) tris(3,5-dimethylpyrazolyl)borate, homocoupling reactions of primary a...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Kealey S,Husbands SM,Bennacef I,Gee AD,Passchier J

更新日期：2014-04-01 00:00:00

abstract：:Steroid oestrogens are typical endocrine-disrupting compounds in the environment and are excreted from the human and animals mainly as conjugates, including sulfate and glucuronide salts. The oestrogen conjugates are largely biologically inactive, but they can be de-conjugated and release free oestrogens, which usuall...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Wang J,Wang Y,Wang T,Cui K,Wang L,Ji R

更新日期：2014-06-15 00:00:00

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：:AZD5122, N-(2-(2,3-difluorobenzylthio)-6-((2R,3R)-3,4-dihydroxybutan-2-ylamino)pyrimidin-4-yl)azetidine-1-sulfonamide was under investigation as a potential chemokine receptor CXCR2 antagonist for the treatment for inflammatory diseases. To gain a better understanding of the human pharmacokinetic profile, an explorato...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Hickey MJ,Allen PH,Kingston LP,Wilkinson DJ

更新日期：2016-05-30 00:00:00

abstract：:Enzalutamide, a second-generation antiandrogen, has been developed for the treatment of castration-resistance prostate cancer. We synthesized the deuterated analogues 6 and found that it showed higher drug exposure and thus stronger antitumor potency in preclinical settings. Compound 6 is being developed clinically fo...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Pang X,Peng L,Chen Y

更新日期：2017-07-01 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：:Targeted delivery of chemotherapeutic drug at the tumor site enhances the efficacy with minimum systemic exposure. Towards this, drugs conjugated with peptides having affinity towards a particular molecular target are recognized as affective agents for targeted chemotherapy. Thus, in the present study, tumor-homing as...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Vats K,Satpati D,Sharma R,Kumar C,Sarma HD,Dash A

更新日期：2017-07-01 00:00:00

abstract：:We synthesized [18 F]trifluoromethyl-l-tryptophan ([18 F]CF3 -l-Trp) using Cu(I)-mediated [18 F]trifluoromethylation to image serotonergic system. Radiochemical yield was 6 ± 1.5% (n = 9), and radiochemical purity was over 99%. The molar activity was 0.44 to 0.76 GBq/μmol. [18 F]CF3 -l-Trp was stable for up to 6 hours...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Kim HY,Lee JY,Lee YS,Jeong JM

更新日期：2019-07-01 00:00:00

abstract：:This study aimed to provide an easy method for synthesis of 1-hydroxy-2-(3-pyridyl) ethylidene bisphosphonic acid monosodium (sod. risedronate) with a high yield of 71%. The synthesized risedronate was labeled with technetium-99 m using two different reducing agents (SnCl2 .2H2 O and NaBH4 ) where NaBH4 gave stable co...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Motaleb MA,Adli AS,El-Tawoosy M,Sanad MH,AbdAllah M

更新日期：2016-04-01 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：:Peptides labeled with short-lived positron emitters are of considerable interest as probes for molecular imaging by positron emission tomography. Herein, the regioselective and convenient radiofluorination of a biologically relevant alkyne-modified SWLAY peptide bound on solid support with the radiolabeling building b...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Pretze M,Mosch B,Bergmann R,Steinbach J,Pietzsch J,Mamat C

更新日期：2014-09-01 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：: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：: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：:[18 F]DCFPyL is a clinical-stage PET radiotracer used to image prostate cancer. This report details the efficient production of [18 F]DCFPyL using single-step direct radiofluorination, without the use of carboxylic acid-protecting groups. Radiolabeling reaction optimization studies revealed an inverse correlation betw...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Dornan MH,Simard JM,Leblond A,Juneau D,Delouya G,Saad F,Ménard C,DaSilva JN

更新日期：2018-05-02 00:00:00

abstract：:[carboxyl-(14) C]Celivarone was synthesised from barium [(14) C]carbonate with overall radiochemical yields in the range 49-53%. The synthetic route involves [(14) C]carbonylation methodology, which both decreased the number of synthetic steps and increased the yields obtained from previous synthetic routes. ...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Whitehead DM,Hartmann S,Ilyas T,Taylor KR,Kohler AD,Ellames GJ

更新日期：2013-02-01 00:00:00

abstract：:Anti-malaria drugs chloroquine and amodiaquine and their metabolites were synthesized to incorporate 13 C and 15 N starting from U-13 C-labeled benzene to give M + 7 isotopomers. Chloroquine and its metabolites were prepared from 7-chloro-1,2,3,4-tetrahydroquinolin-4-one through an aryl substitution with the correspon...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Wu R,Williams RF,Silks LAP,Schmidt JG

更新日期：2019-05-15 00:00:00

abstract：:2 new compounds, L-10503, 2-(3-methoxyphenyl)-5,6-dihydro-s-triazolo [5,1-a] isoquinoline and DL-204 IT, 2-(3-ethoxyphenyl)-5,6-dihydro-s-triazolo [5,1-a] isoquinoline have been developed in the Lepetit Research Laboratories in Milan, Italy. These compounds have been tested in monkeys and rats and have been shown to ...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Sartori G,Consonni P,Omodei-sale A

更新日期：1981-04-01 00:00:00

abstract：:When the isotopic abundance or specific activity of a labeled compound is determined by mass spectrometry (MS), it is necessary to correct the raw MS data to eliminate ion intensity contributions, which arise from the presence of heavy isotopes at natural abundance (e.g., a typical carbon compound contains ~1.1% (13) ...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Schenk DJ,Lockley WJ,Elmore CS,Hesk D,Roberts D

更新日期：2016-04-01 00:00:00

abstract：:Bruton's tyrosine kinase (BTK) is a key component in the B-cell receptor signaling pathway and is consequently a target for in vivo imaging of B-cell malignancies as well as in multiple sclerosis (MS) with positron emission tomography (PET). A recent Phase 2b study with Sanofi's BTK inhibitor, Tolebrutinib (also known...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Dahl K,Turner T,Vasdev N

更新日期：2020-09-01 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：:An agonist PET tracer is of key interest for the imaging of the 5-HT2A receptor, as exemplified by the previously reported success of [11 C]Cimbi-36. Fluorine-18 holds several advantages over carbon-11, making it the radionuclide of choice for clinical purposes. In this respect, an 18 F-labelled agonist 5-HT2A recepto...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Edgar FG,Hansen HD,Leth-Petersen S,Ettrup A,Kristensen JL,Knudsen GM,Herth MM

更新日期：2017-10-01 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：:The worldwide utilization of (68) Ga-radionuclide for the fundamental research and clinical applications is growing exponentially. A broad range of (68) Ga-based imaging agents has been explored during recent years. The development of new clinically useful agents is encouraged by many factors; for example, increasing ...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Velikyan I

更新日期：2015-03-01 00:00:00

abstract：:Pyropheophorbide-a (Pyro) is a promising multifunctional molecule for multimodal tumour imaging and photodynamic therapy, but its clinical applications are seriously restricted by the limited tumour accumulation capability. Here, we designed and synthesized a small-molecule probe that achieved specific dual-modal tumo...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Fan D,Wang K,Gao H,Luo Q,Wang X,Li X,Tong W,Zhang X,Luo C,Yang G,Ai L,Shi J

更新日期：2020-05-15 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：:Herein, we report a short, three-step synthesis of d-[1-(14) C]-serine (4) in high enantiomeric purity. Starting from [(14) C]-KCN and 2-(benzyloxy)acetaldehyde, Strecker reaction using (R)-1-phenylethylamine as the chiral auxiliary gave two diastereomeric aminonitriles 1 and 2 in the ratio of 4:3, which were convenie...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Song F,Salter R,Weaner LE

更新日期：2015-04-01 00:00:00

abstract：:A deeper understanding of the pharmacokinetic and pharmacodynamic properties of a drug candidate is a pivotal component of drug discovery and development. Autoradiography is an excellent technique allowing exploiting the advantages of the use of radioisotopes in the drug disscovery field. The introduction of phosphor ...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Marzorati S,Messina M,Ghiglieri A

更新日期：2019-09-01 00:00:00

abstract：:This open-label, single-period study in healthy subjects estimated evacetrapib absolute bioavailability following simultaneous administration of a 130-mg evacetrapib oral dose and 4-h intravenous (IV) infusion of 175 µg [(13) C8 ]-evacetrapib as a tracer. Plasma samples collected through 168 h were analyzed for evacet...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Cannady EA,Aburub A,Ward C,Hinds C,Czeskis B,Ruterbories K,Suico JG,Royalty J,Ortega D,Pack BW,Begum SL,Annes WF,Lin Q,Small DS

更新日期：2016-05-30 00:00:00

abstract：:Internal therapy with α-emitters should be well suited for micrometastatic disease. Radium-224 emits multiple α-particles through its decay and has a convenient 3.6 days of half-life. Despite its attractive properties, the use of 224 Ra has been limited to bone-seeking applications because it cannot be stably bound to...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Westrøm S,Malenge M,Jorstad IS,Napoli E,Bruland ØS,Bønsdorff TB,Larsen RH

更新日期：2018-05-30 00:00:00