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.


: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 exploratory phase I IV microtracer study was conducted using carbon-14 radiolabelled AZD5122. [(14) C]AZD5122 was carbon-14 labelled in the pyrimidine ring in five steps in an overall radiochemical yield of 19% from [(14) C]thiourea. The absolute oral bioavailability of AZD5122 was assessed in healthy subjects by an oral administration of AZD5122, followed by a concomitant intravenous [(14) C]AZD5122 microdose.


Hickey MJ,Allen PH,Kingston LP,Wilkinson DJ




Has Abstract


2016-05-30 00:00:00












  • Efficient synthesis of deuterium labeled hydroxyzine and aripiprazole.

    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

    pub_type: 杂志文章


    authors: Vohra M,Sandbhor M,Wozniak A

    更新日期:2015-06-15 00:00:00

  • An easy and effective method for synthesis and radiolabelling of risedronate as a model for bone imaging.

    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

    pub_type: 杂志文章


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

    更新日期:2016-04-01 00:00:00

  • Evaluation of [18 F]BR420 and [18 F]BR351 as radiotracers for MMP-9 imaging in colorectal cancer.

    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

    pub_type: 杂志文章


    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

  • Synthesis and application of isotopically labeled flavin nucleotides.

    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

    pub_type: 杂志文章


    authors: Mishanina TV,Kohen A

    更新日期:2015-07-01 00:00:00

  • Enantiomeric radiochemical synthesis of R and S (1-(6-amino-9H-purin-9-yl)-3-fluoropropan-2-yloxy)methylphosphonic acid (FPMPA).

    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

    pub_type: 杂志文章


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

    更新日期:2008-03-13 00:00:00

  • Autoradioluminography, a powerful and reliable tool for drug development: Accelera's experience.

    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

    pub_type: 杂志文章,评审


    authors: Marzorati S,Messina M,Ghiglieri A

    更新日期:2019-09-01 00:00:00

  • Continued rapid growth in (68) Ga applications: update 2013 to June 2014.

    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

    pub_type: 杂志文章,评审


    authors: Velikyan I

    更新日期:2015-03-01 00:00:00

  • Production of [68 Ga]Ga-PSMA: Comparing a manual kit-based method with a module-based automated synthesis approach.

    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

    pub_type: 杂志文章


    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

  • Synthesis of 18 F-radiolabeled diphenyl gallium dithiosemicarbazone using a novel halogen exchange method and in vivo biodistribution.

    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

    pub_type: 杂志文章


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

    更新日期:2019-06-15 00:00:00

  • Exendin-4 analogs in insulinoma theranostics.

    abstract::Insulinomas, neuroendocrine tumors arising from pancreatic beta cells, often show overexpression of the glucagon-like peptide-1 receptor. Therefore, imaging with glucagon-like peptide analog exendin-4 can be used for diagnosis and preoperative localization. This review presents an overview of the development and clini...

    journal_title:Journal of labelled compounds & radiopharmaceuticals

    pub_type: 杂志文章,评审


    authors: Jansen TJP,van Lith SAM,Boss M,Brom M,Joosten L,Béhé M,Buitinga M,Gotthardt M

    更新日期:2019-08-01 00:00:00

  • Synthesis and characterization of 14C-labelled sulfate conjugates of steroid oestrogens.

    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

    pub_type: 杂志文章


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

    更新日期:2014-06-15 00:00:00

  • A three-step radiosynthesis of 6-[(18)  F]fluoro-L-meta-tyrosine starting with [(18)  F]fluoride.

    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

    pub_type: 杂志文章


    authors: Castillo Meleán J,Ermert J,Coenen HH

    更新日期:2015-03-01 00:00:00

  • Withdrawn: The radiosynthesis of novel PI3K inhibitor, 8-ethoxy-2-(4-[18 F] fluorophenyl)-3-nitro-2H-chromene (18 F-EFPNC).

    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 ( The above article, published online on 30 May 2017 on Wiley Online Library (wiley...

    journal_title:Journal of labelled compounds & radiopharmaceuticals

    pub_type: 杂志文章


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

    更新日期:2020-12-01 00:00:00

  • An efficient method for synthesizing dimethylsulfonio-34 S-propionate hydrochloride from 34 S8.

    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

    pub_type: 杂志文章


    authors: Wirth JS,Whitman WB

    更新日期:2019-01-01 00:00:00

  • 99m Tc-labeled NGR-chlorambucil conjugate, 99m Tc-HYNIC-CLB-c(NGR) for targeted chemotherapy and molecular imaging.

    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

    pub_type: 杂志文章


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

    更新日期:2017-07-01 00:00:00

  • An alternative and robust synthesis of [(13) C4 ]Baraclude® (entecavir).

    abstract::Stable isotope-labeled [(13) C4 ]entecavir (1) was prepared in 11 steps. Commercially available [(13) C]guanidine hydrochloride and diethyl[1,2,3-(13) C3 ]malonate were condensed to yield 2-amino[2,4,5,6-(13) C4 ]pyrimidine-4,6-diol (8). This was converted to the desired purine (7) in five steps. Introduction of the c...

    journal_title:Journal of labelled compounds & radiopharmaceuticals

    pub_type: 杂志文章


    authors: Easter JA,Burrell RC,Bonacorsi SJ Jr

    更新日期:2013-10-01 00:00:00

  • The synthesis of 2 14C-labelled 2-(3-alkoxyphenyl)-5,6-dihydro-5-trazolo[5, 1-a] isoquinoline compounds, novel antifertility agents.

    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

    pub_type: 杂志文章


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

    更新日期:1981-04-01 00:00:00

  • Simplified and robust one-step radiosynthesis of [18 F]DCFPyL via direct radiofluorination and cartridge-based purification.

    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

    pub_type: 杂志文章


    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

  • Radiolabelling of steroids: the synthesis of 17α-[4-(14) C]trenbolone.

    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

    pub_type: 杂志文章


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

    更新日期:2013-07-01 00:00:00

  • Preparation of a novel radiotracer targeting the EphB4 receptor via radiofluorination using spiro azetidinium salts as precursor.

    abstract::The visualization of Eph receptors, which are overexpressed in various tumor entities, using selective small molecule Eph inhibitors by means of positron emission tomography is a promising approach for tumor imaging. N-(Pyrimidinyl)indazolamines represent a class of compounds, which are known to have high affinity esp...

    journal_title:Journal of labelled compounds & radiopharmaceuticals

    pub_type: 杂志文章


    authors: Wiemer J,Steinbach J,Pietzsch J,Mamat C

    更新日期:2017-08-01 00:00:00

  • Synthesis of [15 N]-cholamine bromide hydrobromide.

    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

    pub_type: 杂志文章


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

    更新日期:2018-04-01 00:00:00

  • Synthesis of [3α-(3) H] 17α-hydroxy pregnenolone and [3α-(3) H] pregnenolone.

    abstract::For the first time, [3α-(3) H] 17α-hydroxy pregnenolone (1) was synthesized through a multiple step sequence. The presence of [3β-(3) H] isomer in RP-HPLC purified product was identified by tritium NMR. The [3β-(3) H] isomer was then separated from [3α-(3) H] 17α-hydroxy pregnenolone with chiralPAK AD-H column. [3α-(3...

    journal_title:Journal of labelled compounds & radiopharmaceuticals

    pub_type: 杂志文章


    authors: Tian Y,Hong Y,Bonacorsi SJ,Balog A,Gong S

    更新日期:2014-01-01 00:00:00

  • Automated synthesis and purification of [18F]fluoro-[di-deutero]methyl tosylate.

    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

    pub_type: 杂志文章


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

    更新日期:2013-06-15 00:00:00

  • 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::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

    pub_type: 杂志文章


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

    更新日期:2019-07-01 00:00:00

  • The magic of small structure differences in a sodium-glucose cotransporter drug discovery project-14 C-labelled drug candidates in a key-differentiating study.

    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

    pub_type: 杂志文章


    authors: Schudok M,Glombik H,Derdau V

    更新日期:2020-07-07 00:00:00

  • Absolute bioavailability of evacetrapib in healthy subjects determined by simultaneous administration of oral evacetrapib and intravenous [(13) C8 ]-evacetrapib as a tracer.

    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

    pub_type: 临床试验,杂志文章


    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

  • Synthesis of (3) H, (2) H4 and (14) C-SCH 417690 (Vicriviroc).

    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

    pub_type: 杂志文章


    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

  • Tropane-derived (11) C-labelled and (18) F-labelled DAT ligands.

    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

    pub_type: 杂志文章,评审


    authors: Riss PJ,Stockhofe K,Roesch F

    更新日期:2013-03-01 00:00:00

  • Development of a 68 Ga-labelled PET tracer for carbonic anhydrase IX-overexpressed tumors using the artificial sweetener saccharin.

    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

    pub_type: 杂志文章


    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

  • Fully automated radiosynthesis of [1-(2-[18 F]fluoroethyl),1H[1,2,3]triazole 4-ethylene] triphenylphosphonium bromide as a potential positron emission tomography tracer for imaging apoptosis.

    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

    pub_type: 杂志文章


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

    更新日期:2013-05-30 00:00:00