A comparison of four PET tracers for brain hypoxia mapping in a rodent model of stroke.

Abstract:

INTRODUCTION:Severe brain hypoxia in the territory of the occluded artery is a key feature of ischemic stroke. This region can be imaged using positron emission tomography (PET) and the standard hypoxia radiotracer (18)F-fluoromisonidazole ((18)F-FMISO). However, the utility of (18)F-FMISO is limited by its slow accumulation in the lesion. Therefore, this study investigated three hypoxia-sensitive radiotracers, namely the nitroimidazole (18)F-fluoroazomycin arabinoside ((18)F-FAZA) and two (64)Cu bis(thiosemicarbazone) complexes ((64)Cu-ATSM and (64)Cu-ATSE), expected to have improved pharmacokinetic profiles relative to (18)F-FMISO, in a rodent model of ischemic stroke. METHODS:In anaesthetised Wistar rats, the distal middle cerebral artery was permanently occluded by electrocoagulation, the radiotracers administered intravenously and animals PET scanned for up to 3hours, followed by T2-weighted magnetic resonance imaging to map the infarct. RESULTS:As expected, late and prominent (18)F-FMISO retention was observed despite lower tracer delivery into the affected region. Time-activity curves revealed that both (64)Cu-ATSM and (64)Cu-ATSE showed rapid entry and efflux from the brain, but did not show significant accumulation in the lesion. (18)F-FAZA showed limited brain penetration, and accumulation in the lesion was inconsistent, low and as slow as (18)F-FMISO. CONCLUSIONS:This study suggests further development of these radiotracers as hypoxia markers for ischemic stroke may not be warranted.

journal_name

Nucl Med Biol

authors

Williamson DJ,Ejaz S,Sitnikov S,Fryer TD,Sawiak SJ,Burke P,Baron JC,Aigbirhio FI

doi

10.1016/j.nucmedbio.2012.11.012

subject

Has Abstract

pub_date

2013-04-01 00:00:00

pages

338-44

issue

3

eissn

0969-8051

issn

1872-9614

pii

S0969-8051(12)00309-5

journal_volume

40

pub_type

杂志文章
  • Investigation of a potential scintigraphic marker of apoptosis: radioiodinated Z-Val-Ala-DL-Asp(O-methyl)-fluoromethyl ketone.

    abstract::The imaging of apoptosis represents an attractive diagnostic goal in the area of tumor therapy, degenerative diseases and organ transplantation. Since caspases play a key role during the early period of the intracellular signal cascade of cells undergoing apoptosis we considered benzyloxycarbonyl-Val-Ala-DL-Asp(O-meth...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(01)00247-5

    authors: Haberkorn U,Kinscherf R,Krammer PH,Mier W,Eisenhut M

    更新日期:2001-10-01 00:00:00

  • The human polynucleotide kinase/phosphatase (hPNKP) inhibitor A12B4C3 radiosensitizes human myeloid leukemia cells to Auger electron-emitting anti-CD123 ¹¹¹In-NLS-7G3 radioimmunoconjugates.

    abstract:INTRODUCTION:Leukemia stem cells (LSCs) are believed to be responsible for initiating and propagating acute myeloid leukemia (AML) and for causing relapse after treatment. Radioimmunotherapy (RIT) targeting these cells may improve the treatment of AML, but is limited by the low density of target epitopes. Our objective...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2014.02.003

    authors: Zereshkian A,Leyton JV,Cai Z,Bergstrom D,Weinfeld M,Reilly RM

    更新日期:2014-05-01 00:00:00

  • Improved radioiodination of biomolecules using exhaustive Chloramine-T oxidation.

    abstract::To improve standardization in analytical reagents we investigated Chloramine-T radioiodination (125I) of several biomolecules based on the use of a single amount of the oxidizing agent Chloramine-T as the limiting reagent being exhausted during the course of the reaction. Whenever the labeling yield resulted in less t...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(01)00261-x

    authors: Robles AM,Balter HS,Oliver P,Welling MM,Pauwels EK

    更新日期:2001-11-01 00:00:00

  • Biodistribution of 3,4-dihydro-5-[11C]methoxy-1(2H)-isoquinolinone, a potential PET tracer for poly(ADP-ribose) synthetase.

    abstract::Poly(adenosine diphosphate-ribose) synthetase (PARS) is a nuclear enzyme that is activated by deoxyribonucleic acid (DNA) strand breaks and participates in DNA repair. Excessive PARS activation, however, leads to cell death due to depletion of adenosine triphosphate (ATP). To evaluate whether it is possible to detect ...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(00)00146-3

    authors: Miyake Y,Kuge Y,Shimadzu H,Hashimoto N,Ishida Y,Shibakawa M,Nishimura T

    更新日期:2000-11-01 00:00:00

  • PET FDG studies in oncology.

    abstract::Positron emission tomography (PET) studies of cancer with the glucose analog 2-[F-18]fluoro-2-deoxy-D-glucose (FDG) have emerged as both a useful research and clinical method for detecting (diagnosing), staging, and monitoring treatment responses in a variety of neoplasms, including tumors of the brain, head and neck,...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/0969-8051(94)90045-0

    authors: Hawkins RA,Hoh CK

    更新日期:1994-07-01 00:00:00

  • Cellular distribution of 111In-LDTPA galactose BSA in normal and asialoglycoprotein receptor-deficient mouse liver.

    abstract::111In-LDTPA galactose BSA (bovine serum albumin) was used to evaluate the asialoglycoprotein receptor (ASGPR) system in both normal and ASGPR-deficient mice. The radiolabeled glycoprotein had complete liver uptake in both normal and ASGPR-deficient mice. Metabolism and hepatic cell-type distribution studies were perfo...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(97)00222-9

    authors: Deal KA,Cristel ME,Welch MJ

    更新日期:1998-05-01 00:00:00

  • Synthesis and properties of 18F-labeled potential myocardial blood flow tracers.

    abstract::PET centers without particle accelerators make clinical PET widely available at reduced cost. For myocardial perfusion tracers, these satellite PET centers are limited to generator- produced 82Rb(+) and 62Cu[PTSM]. Their limitations motivate a search for transportable alternatives. In search of new tracers we have syn...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(01)00233-5

    authors: Studenov AR,Berridge MS

    更新日期:2001-08-01 00:00:00

  • 131I-labeled chitosan hydrogels for radioembolization: A preclinical study in small animals.

    abstract:INTRODUCTION:The purpose of the study was to examine potential of 131I-labeled chitosan hydrogels (Chi) for treatment of liver cancer. METHODS:Orthotopic hepatoma was induced by McA-RH7777-fLuc cells (1×107) that were injected into the left hepatic lobe of rats. Ten days later, tumor-bearing rats evidenced by biolumin...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2017.05.006

    authors: Hwang H,Kim KI,Kwon J,Kim BS,Jeong HS,Jang SJ,Oh PS,Park HS,Lim ST,Sohn MH,Jeong HJ

    更新日期:2017-09-01 00:00:00

  • 99Mo/(99m)Tc separation: an assessment of technology options.

    abstract::Several strategies for the effective separation of (99m)Tc from (99)Mo have been developed and validated. Due to the success of column chromatographic separation using acidic alumina coupled with high specific activity fission (99)Mo (F (99)Mo) for production of (99)Mo/(99m)Tc generators, however, most technologies un...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章,评审

    doi:10.1016/j.nucmedbio.2012.10.005

    authors: Dash A,Knapp FF Jr,Pillai MR

    更新日期:2013-02-01 00:00:00

  • Physical optimization of production by deuteron irradiation of high specific activity (177g)Lu suitable for radioimmunotherapy.

    abstract::Deuteron-induced nuclear reactions for generation of no-carrier-added (NCA) Lu isotopes were investigated using the stacked-foil activation technique on natural Yb targets at energies up to Ed=18.18MeV. The decay curve of ¹⁷⁷Yb, the growth curve of the cumulative (direct and indirect) and the direct production of (177...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2014.02.007

    authors: Manenti S,Bonardi ML,Gini L,Groppi F

    更新日期:2014-05-01 00:00:00

  • Humanized versus murine anti-human epidermal growth factor receptor monoclonal antibodies for immunoscintigraphic studies.

    abstract::The anti-human epidermal growth factor receptor (EGF-R) humanized antibody h-R3 (IgG(1)), which binds to an extracellular domain of EGF-R, was used to evaluate the biodistribution on nude mice xenografted with A431 epidermoid carcinoma cell line. Results are compared with its murine version ior egf/r3 monoclonal antib...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(99)00094-3

    authors: Morales AA,Ducongé J,Alvarez-Ruiz D,Becquer-Viart ML,Núñez-Gandolff G,Fernández E,Caballero-Torres I,Iznaga-Escobar N

    更新日期:2000-02-01 00:00:00

  • Pharmacokinetic computer simulations of the relationship between in vivo and in vitro neuroreceptor subtype selectivity of radioligands.

    abstract::Pharmacokinetic computer simulations reveal a discrepancy between the in vivo and in vitro neuroreceptor subtype selectivity of radioligands. For radioligands with an in vitro neuroreceptor subtype selectivity between 0.1 and 10.0, the in vivo neuroreceptor subtype selectivity appears to be constrained to be between 0...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(99)00061-x

    authors: Zeeberg BR

    更新日期:1999-10-01 00:00:00

  • Desferrioxamine as an appropriate chelator for 90Nb: comparison of its complexation properties for M-Df-Octreotide (M = Nb, Fe, Ga, Zr).

    abstract::The niobium-90 radioisotope ((90)Nb) holds considerable promise for use in immuno-PET, due to its decay parameters (t½ = 14.6h, positron yield=53%, Eß(+)(mean) = 0.35 MeV and Eß(+)(max) = 1.5 MeV). In particular, (90)Nb appears well suited to detect in vivo the pharmacokinetics of large targeting vectors (50-150 kDa)....

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2014.06.006

    authors: Radchenko V,Busse S,Roesch F

    更新日期:2014-10-01 00:00:00

  • Propionyl-L-carnitine: labelling in the N-methyl position with carbon-11 and pharmacokinetic studies in rats.

    abstract::The prospective therapeutic, propionyl-L-carnitine, was labelled in the N-methyl position with the positron-emitter, carbon-11 (t1/2 = 20.4 min), with a view to studying its pharmacokinetics in humans using PET. Labelling was achieved by methylating nor-propionyl-L-carnitine hydrochloride with no-carrier-added [11C]io...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/0969-8051(95)00010-u

    authors: Davenport RJ,Law MP,Pike VW,Osman S,Poole KG

    更新日期:1995-08-01 00:00:00

  • Synthesis of O-(2-[18F]fluoroethyl)-L-tyrosine based on a cartridge purification method.

    abstract:INTRODUCTION:O-(2-[(18)F]fluoroethyl)-L-tyrosine (FET) is widely used as a positron emission tomography tracer for brain tumors. Usually, a high-performance liquid chromatography (HPLC) purification at the end of the two-step synthesis is applied. In this work, we report an automatic radiosynthesis of FET with a purifi...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2011.01.006

    authors: Mueller D,Klette I,Kalb F,Baum RP

    更新日期:2011-07-01 00:00:00

  • Preliminary assessment of extrastriatal dopamine D-2 receptor binding in the rodent and nonhuman primate brains using the high affinity radioligand, 18F-fallypride.

    abstract::We have identified the value of 18F-fallypride [(S)-N-[(1-allyl-2-pyrrolidinyl)methyl]-5-(3-[18F]fluoropropyl)-2, 3-dimethoxybenzamide], as a dopamine D-2 receptor radiotracer for the study of striatal and extrastriatal receptors. Fallypride exhibits high affinities for D-2 and D-3 subtypes and low affinity for D-4 (3...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(99)00012-8

    authors: Mukherjee J,Yang ZY,Brown T,Lew R,Wernick M,Ouyang X,Yasillo N,Chen CT,Mintzer R,Cooper M

    更新日期:1999-07-01 00:00:00

  • Synthesis and fluorine-18 radiolabeling of a phospholipid as a PET imaging agent for prostate cancer.

    abstract:INTRODUCTION:Altered lipid metabolism and subsequent changes in cellular lipid composition have been observed in prostate cancer cells, are associated with poor clinical outcome, and are promising targets for metabolic therapies. This study reports for the first time on the synthesis of a phospholipid radiotracer based...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2020.11.007

    authors: Kwan KH,Burvenich IJG,Centenera MM,Goh YW,Rigopoulos A,Dehairs J,Swinnen JV,Raj GV,Hoy AJ,Butler LM,Scott AM,White JM,Ackermann U

    更新日期:2020-11-28 00:00:00

  • Biodistribution of (125)I-labeled anti-endoglin antibody using SPECT/CT imaging: Impact of in vivo deiodination on tumor accumulation in mice.

    abstract:INTRODUCTION:Radiolabeled antibodies directed against endoglin (CD105) are promising tools for imaging and antiangiogenic cancer therapy. To validate iodinated antibodies as reliable tracers, we investigated the influence of the radiolabeling method (direct or indirect) on their in vivo stability. METHODS:Anti-CD105 m...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2016.03.007

    authors: Karmani L,Levêque P,Bouzin C,Bol A,Dieu M,Walrand S,Vander Borght T,Feron O,Grégoire V,Bonifazi D,Michiels C,Lucas S,Gallez B

    更新日期:2016-07-01 00:00:00

  • Synthesis and evaluation of an 18F-labeled dopa prodrug as a PET tracer for studying brain dopamine metabolism.

    abstract::In the quantitative studies of presynaptic dopamine metabolism by PET with 6-[18F]fluoro-L-dopa (6-[18F]FDOPA), metabolic analysis in the plasma is required to determine the precise input function because of susceptibility of the compound to peripheral metabolism. In this study, we prepared 6-[18F]-fluoro-O-pivaloyl-L...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/0969-8051(95)02083-7

    authors: Ishiwata K,Shinoda M,Ishii S,Nozaki T,Senda M

    更新日期:1996-04-01 00:00:00

  • Synthesis, in vitro and in vivo characterization of novel 99mTc-'4+1'-labeled 5-nitroimidazole derivatives as potential agents for imaging hypoxia.

    abstract:UNLABELLED:The evaluation of oxygenation status of solid tumors is an important field of radiopharmaceutical research. With the aim to develop new potential 99mTc-radiopharmaceuticals for imaging hypoxia, we have synthesized two novel isocyanide derivatives of metronidazole, which has demonstrated high affinity for hyp...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2011.12.012

    authors: Giglio J,Fernández S,Pietzsch HJ,Dematteis S,Moreno M,Pacheco JP,Cerecetto H,Rey A

    更新日期:2012-07-01 00:00:00

  • Cellular penetration and nuclear importation properties of 111In-labeled and 123I-labeled HIV-1 tat peptide immunoconjugates in BT-474 human breast cancer cells.

    abstract:INTRODUCTION:Our objective was to compare the cell penetration and nuclear importation properties of 111In-labeled and 123I-labeled immunoconjugates (ICs) composed of 16-mer peptides (GRKKRRQRRRPPQGYG) derived from HIV-1 transactivator of transcription (tat) protein and anti-mouse IgG (mIgG) in BT-474 breast cancer (BC...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2006.10.008

    authors: Cornelissen B,Hu M,McLarty K,Costantini D,Reilly RM

    更新日期:2007-01-01 00:00:00

  • Evaluation of [11C]laniquidar as a tracer of P-glycoprotein: radiosynthesis and biodistribution in rats.

    abstract::At present, P-glycoprotein (P-gp) function can be studied using positron emission tomography (PET) together with a labelled P-gp substrate such as R-[11C]verapamil. Such a tracer is, however, less suitable for investigating P-gp (over)expression. Laniquidar is a third-generation P-gp inhibitor, which has been used in ...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2009.03.004

    authors: Luurtsema G,Schuit RC,Klok RP,Verbeek J,Leysen JE,Lammertsma AA,Windhorst AD

    更新日期:2009-08-01 00:00:00

  • Dual radiolabeled liposomes: biodistribution studies and localization of focal sites of infection in rats.

    abstract::Liposomes encapsulating both glutathione and deferoxamine were labeled with 99mTc-HMPAO and 111In-oxine at the same time. These dual radiolabeled liposomes were intravenously injected in rats with S. aureus infection in thigh. The target-to-background ratio (T/BG) increased from 2.9 at 2 h to 4.4 at 8 h in 99mTc image...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(97)00162-5

    authors: Awasthi VD,Goins B,Klipper R,Phillips WT

    更新日期:1998-02-01 00:00:00

  • Preliminary studies of 99mTc-BnAO and its analogues: synthesis, radiolabeling and in vitro cell uptake.

    abstract:INTRODUCTION:(99m)Tc-BnAO is one of the nonnitroimidazole hypoxia markers with the highest citation and could be potentially useful in both oncology and other clinical applications. However, it appears inferior in vitro due to lower absolute accumulation and smaller anoxic/normoxic uptake ratio. It is possible that the...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2009.09.003

    authors: Sun X,Chu T,Wang X

    更新日期:2010-02-01 00:00:00

  • The peripheral benzodiazepine receptor ligand PK11195 binds with high affinity to the acute phase reactant alpha1-acid glycoprotein: implications for the use of the ligand as a CNS inflammatory marker.

    abstract::The peripheral benzodiazepine receptor ligand PK11195 has been used as an in vivo marker of neuroinflammation in positron emission tomography studies in man. One of the methodological issues surrounding the use of the ligand in these studies is the highly variable kinetic behavior of [(11)C]PK11195 in plasma. We there...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(02)00410-9

    authors: Lockhart A,Davis B,Matthews JC,Rahmoune H,Hong G,Gee A,Earnshaw D,Brown J

    更新日期:2003-02-01 00:00:00

  • Evaluation of nigrostriatal damage and its change over weeks in a rat model of Parkinson's disease: small animal positron emission tomography studies with [(11)C]beta-CFT.

    abstract:INTRODUCTION:The cardinal pathological feature of Parkinson's disease (PD) is progressive loss of dopaminergic neurons. Since dopamine transporter (DAT) is a protein located presynaptically on dopaminergic nerve terminals, radioligands that bind to these sites are promising radiopharmaceuticals for evaluation of the in...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2009.06.005

    authors: Liu L,Wang Y,Li B,Jia J,Sun Z,Zhang J,Tian J,Wang X

    更新日期:2009-11-01 00:00:00

  • PET measurement of "GABA shift" in the rat brain: A preclinical application of bolus plus constant infusion paradigm of [18F]flumazenil.

    abstract:INTRODUCTION:We measured the tiagabine-induced enhancement of the GABAA receptor's affinity for benzodiazepine ligands ("GABA shift") using [18F]flumazenil (FMZ) PET with preclinical application of bolus plus constant infusion (B/I). Differences in quantified results of [18F]FMZ binding were compared to that of [18F]FM...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2016.11.003

    authors: Kim W,Park HS,Moon BS,Lee BC,Kim SE

    更新日期:2017-02-01 00:00:00

  • Production of Zr-89 using sputtered yttrium coin targets 89Zr using sputtered yttrium coin targets.

    abstract::An increasing interest in zirconium-89 (89Zr) can be attributed to the isotope's half-life which is compatible with antibody imaging using positron emission tomography (PET). The goal of this work was to develop an efficient means of production for 89Zr that provides this isotope with high radionuclidic purity and spe...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2017.03.004

    authors: Queern SL,Aweda TA,Massicano AVF,Clanton NA,El Sayed R,Sader JA,Zyuzin A,Lapi SE

    更新日期:2017-07-01 00:00:00

  • Evaluation of in vivo selective binding of [11C]doxepin to histamine H1 receptors in five animal species.

    abstract::The specific binding of [(11)C]doxepin, which has been used as a radioligand for mapping histamine H(1) receptors in human brain by positron emission tomography, was evaluated in five animal species. In mice the [(11)C]doxepin uptake was reduced by treatment with cold doxepin and two H(1) receptor antagonists, but not...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2003.11.005

    authors: Ishiwata K,Kawamura K,Wang WF,Tsukada H,Harada N,Mochizuki H,Kimura Y,Ishii K,Iwata R,Yanai K

    更新日期:2004-05-01 00:00:00

  • Liver distribution of 99mTc-DL-homocysteine in experimental hepatitis rats.

    abstract::Liver accumulation of 99mTc-DL-homocysteine (99mTc-Hcy), which had been found to accumulate in several experimental tumors, was studied using experimental hepatitis models of rats. The distribution of this compound in liver of rats treated with CCl4 (25-100 microL/100 g body weight) was more than five times higher tha...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/0969-8051(93)90091-8

    authors: Takeda A,Okumura H,Okada S

    更新日期:1993-11-01 00:00:00