The synthesis of [(14) C]AZD5122. Incorporation of an IV (14) C-microtracer dose into a first in human study to determine the absolute oral bioavailability of AZD5122.

abstract：:Ulcerative colitis is a chronic disease having a regressive nature. Commonly used diagnostic methods have the disadvantage to be invasive, time-consuming, and expensive. Therefore, a new sensitive method for the detection and monitoring of disease activity is urgently needed in clinical practice. In the current invest...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： El-Kawy OA,Ibrahim IT,Farah K

更新日期：2015-06-30 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：: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 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：:Vicriviroc or SCH 417690 is a potent and selective antagonist of the CCR5 receptor. CCR5 receptor antagonists have the potential for the treatment of HIV infections. Four distinct isotopically labelled forms of SCH 417690 were synthesized. Low specific activity [(3) H]SCH 417690 was prepared for a preliminary absorpti...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Hesk D,Borges S,Hendershot S,Koharski D,McNamara P,Ren S,Saluja S,Truong V,Voronin K

更新日期：2016-05-15 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：:Molecular imaging of tumour tissue focusses mainly on extracellular epitopes such as tumour angiogenesis or signal transduction receptors expressed on the cell membrane. However, most biological processes that define tumour phenotype occur within the cell. In this mini-review, an overview is given of the various techn...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Cornelissen B

更新日期：2014-04-01 00:00:00

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：: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：: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：:The radiosynthesis of 6-[(18)  F]fluoro-L-m-tyrosine has generally been performed by electrophilic radiofluorination, which exhibits several drawbacks. In the present work, a three-step radiochemical synthesis is described starting from [(18)  F]fluoride. The synthetic sequence, including isotopic exchange, Baeyer-Vil...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Castillo Meleán J,Ermert J,Coenen HH

更新日期：2015-03-01 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：:Therapy for human immunodeficiency virus (HIV)-infected patients requires chronic multidrug administration. The eventual failure of therapy in some patients has brought into question the tissue concentration of the drugs. With an appropriately radiolabeled compound, we could utilize positron emission tomography to pro...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Kiesewetter DO,Knudson K,Collins M,Srinivasula S,Lim E,Di Mascio M

更新日期：2008-03-13 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：: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：: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：: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：:17β-Hydroxyestra-4,9,11-trien-3-one or trenbolone is an anabolic steroid used in some meat producing countries where its use is licenced. In cattle it is metabolised into 17α-trenbolone. We were required to make 17α-[4-(14) C]trenbolone for use in environmental fate studies. At the same time we also had a request to m...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Hendry D,Knagg E,Smith NA,Woolley GT

更新日期：2013-07-01 00:00:00

abstract：:Cancer is one of the leading causes of human death, and early detection can be beneficial for its timely therapy and management. For the early detection of cancer, positron emission tomography (PET) is more accurate and sensitive than other imaging modalities, such as computed tomography and magnetic resonance imaging...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Alauddin MM

更新日期：2013-03-01 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：:Cell membrane association of proteins can be achieved by the addition of lipid moieties to the polypeptide chain, and such lipid-modified proteins have important biological functions. A class of cell surface proteins contains a complex glycosylphosphatidylinositol (GPI) glycolipid at the C-terminus, and they are accum...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Schäfer B,Orbán E,Kele Z,Tömböly C

更新日期：2015-01-01 00:00:00

abstract：:Huisgen cycloaddition is attractive to label peptide because of its rapidity and bioorthogonality. However, for larger tracers, the physico-chemical differences between the precursor and the tracer are usually insufficient to allow their separation by HPLC, reducing the specific activity. This is of importance for pep...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： George GP,Pisaneschi F,Stevens E,Nguyen QD,Åberg O,Spivey AC,Aboagye EO

更新日期：2013-11-01 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：: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：: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：: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：: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：: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

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：:Automated synthetic procedures of [(18)F]fluoro-[di-deutero]methyl tosylate on a GE TRACERlab FX F-N module and a non-commercial synthesis module have been developed. The syntheses included azeotropic drying of the [(18)F]fluoride, nucleophilic (18)F-fluorination of bis(tosyloxy)-[di-deutero]methane, HPLC purification...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Beyerlein F,Piel M,Höhnemann S,Rösch F

更新日期：2013-06-15 00:00:00