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 [68 Ga]Ga-DOTA-K-A9 could detect a staphylococcal infection in vivo and distinguish it from aseptic inflammation. An optimized [68 Ga]Ga-DOTA-K-A9 synthesis omitting the use of acetone was developed, yielding 93 ± 0.9% radiochemical purity. The in vivo infection binding specificity of [68 Ga]Ga-DOTA-K-A9 was evaluated by micro positron emission tomography/magnetic resonance imaging of 15 mice with either subcutaneous Staphylococcus aureus infection or turpentine-induced inflammation and compared with 2-deoxy-2-[18 F]fluoro-D-glucose ([18 F]FDG). The scans showed that [68 Ga]Ga-DOTA-K-A9 accumulated in all the infected mice at injected doses ≥3.6 MBq. However, the tracer was not found to be selective towards infection, since the [68 Ga]Ga-DOTA-K-A9 also accumulated in mice with inflammation. In a concurrent in vitro binding evaluation performed with a 5-carboxytetramethylrhodamine (TAMRA) fluorescence analogue of the peptide, TAMRA-K-A9, the microscopy results suggested that TAMRA-K-A9 bound to an intracellular epitope and therefore preferentially targeted dead bacteria. Thus, the [68 Ga]Ga-DOTA-K-A9 uptake observed in vivo is presumably a combination of local hyperemia, vascular leakiness and/or binding to an epitope present in dead bacteria.
journal_name
J Labelled Comp Radiopharmjournal_title
Journal of labelled compounds & radiopharmaceuticalsauthors
Nielsen KM,Jørgensen NP,Kyneb MH,Borghammer P,Meyer RL,Thomsen TR,Bender D,Jensen SB,Nielsen OL,Alstrup AKOdoi
10.1002/jlcr.3640subject
Has Abstractpub_date
2018-05-23 00:00:00eissn
0362-4803issn
1099-1344pub_type
杂志文章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
pub_type： 杂志文章
doi：10.1002/jlcr.3385
更新日期：2016-05-30 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
pub_type： 杂志文章
doi：10.1002/jlcr.1414
更新日期：2007-07-17 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
pub_type： 杂志文章
doi：10.1002/jlcr.3597
更新日期：2018-04-01 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
pub_type： 杂志文章,评审
doi：10.1002/jlcr.3562
更新日期：2018-03-01 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
pub_type： 杂志文章
doi：10.1002/jlcr.3476
更新日期：2017-01-01 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
pub_type： 杂志文章
doi：10.1002/jlcr.3879
更新日期：2020-11-01 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
pub_type： 杂志文章
doi：10.1002/jlcr.3237
更新日期：2014-09-01 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
pub_type： 杂志文章,评审
doi：10.1002/jlcr.3003
更新日期：2013-03-01 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
pub_type： 杂志文章
doi：10.1002/jlcr.3721
更新日期：2019-05-15 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
pub_type： 杂志文章
doi：10.1002/jlcr.3387
更新日期：2016-05-15 00:00:00
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
doi：10.1002/jlcr.3064
更新日期：2013-10-01 00:00:00
abstract：:As part of a program toward making analogues of amlexanox (1), currently under clinical investigation for the treatment of type 2 diabetes and obesity, we have synthesized derivative 5 in which deuterium has been introduced into two sites of metabolism on the C-7 isopropyl function of amlexanox. The synthesis of 5 was...
journal_title：Journal of labelled compounds & radiopharmaceuticals
pub_type： 杂志文章
doi：10.1002/jlcr.3716
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
pub_type： 杂志文章
doi：10.1002/jlcr.3869
更新日期：2020-07-07 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
pub_type： 杂志文章
doi：10.1002/jlcr.3431
更新日期：2016-09-01 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
pub_type： 杂志文章
doi：10.1002/jlcr.3168
更新日期：2014-02-01 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
pub_type： 杂志文章
doi：10.1002/jlcr.3746
更新日期：2019-06-15 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
pub_type： 杂志文章
doi：10.1002/jlcr.3598
更新日期：2018-04-01 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
pub_type： 杂志文章
doi：10.1002/jlcr.1505
更新日期：2008-03-13 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
pub_type： 杂志文章,评审
doi：10.1002/jlcr.3250
更新日期：2015-03-01 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
pub_type： 杂志文章
doi：10.1002/jlcr.3699
更新日期：2019-11-01 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
pub_type： 杂志文章
doi：10.1002/jlcr.3209
更新日期：2014-06-15 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
pub_type： 杂志文章
doi：10.1002/jlcr.3213
更新日期：2014-06-30 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
pub_type： 杂志文章
doi：10.1002/jlcr.3089
更新日期：2013-07-01 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
pub_type： 杂志文章
doi：10.1002/jlcr.3696
更新日期：2019-01-01 00:00:00
abstract：:The syntheses of perdeuterated phytoalexins nasturlexins A and C, and putative biosynthetic precursors, including phenylethyl isothiocyanates and phenylethyl dithiocarbamates, using commercially available [2,3,4,5,6-D5 ]phenylalanine, [2,3,4,5,6-D5 ]nitrobenzene, and [2,3,4,5,6-D5 ]benzaldehyde are described. In addit...
journal_title：Journal of labelled compounds & radiopharmaceuticals
pub_type： 杂志文章
doi：10.1002/jlcr.3591
更新日期：2018-02-01 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
pub_type： 杂志文章
doi：10.1002/jlcr.3522
更新日期：2017-07-01 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
pub_type： 杂志文章,评审
doi：10.1002/jlcr.3158
更新日期：2014-04-01 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
pub_type： 杂志文章
doi：10.1002/jlcr.3384
更新日期：2016-04-01 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
pub_type： 杂志文章
doi：10.1002/jlcr.3272
更新日期：2015-04-01 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
pub_type： 杂志文章,评审
doi：10.1002/jlcr.3152
更新日期：2014-04-01 00:00:00
