当前位置： SCI文献检索 > NUCLEAR MEDICINE AND BIOLOGY期刊下所有文献 > Astatine-211 labeled anti-HER2 5F7 single domain antibody fragment conjugates: radiolabeling and preliminary evaluation.

Astatine-211 labeled anti-HER2 5F7 single domain antibody fragment conjugates: radiolabeling and preliminary evaluation.

Abstract：

INTRODUCTION:Derived from heavy chain only camelid antibodies, ~15-kDa single-domain antibody fragments (sdAbs) are an attractive platform for developing molecularly specific imaging probes and targeted radiotherapeutics. The rapid tumor accumulation and normal tissue clearance of sdAbs might be ideal for use with 211At, a 7.2-h half-life α-emitter, if appropriate labeling chemistry can be devised to trap 211At in cancer cells after sdAb binding. This study evaluated two reagents, [211At]SAGMB and iso-[211At]SAGMB, for this purpose. METHODS:[211At]SAGMB and iso-[211At]SAGMB, and their radioiodinated analogues [131I]SGMIB and iso-[131I]SGMIB, were synthesized by halodestannylation and reacted with the anti-HER2 sdAb 5F7. Radiochemical purity, immunoreactivity and binding affinity were determined. Paired-label internalization assays on HER2-expressing BT474M1 breast carcinoma cells directly compared [131I]SGMIB-5F7/[211At]SAGMB-5F7 and iso-[131I]SGMIB-5F7/iso-[211At]SAGMB-5F7 tandems. The biodistribution of the two tandems was evaluated in SCID mice with subcutaneous BT474M1 xenografts. RESULTS:Radiochemical yields for Boc2-iso-[211At]SAGMB and Boc2-[211At]SAGMB synthesis, and efficiencies for coupling of iso-[211At]SAGMB and [211At]SAGMB to 5F7 were similar, with radiochemical purities of [211At]SAGMB-5F7 and iso-[211At]SAGMB-5F7 >98%. iso-[211At]SAGMB-5F7 and [211At]SAGMB-5F7 had immunoreactive fractions >80% and HER2 binding affinities of less than 5 nM. Internalization assays demonstrated high intracellular trapping of radioactivity, with little difference observed between corresponding 211At- and 131I-labeled 5F7 conjugates. Higher BT474M1 intracellular retention was observed from 1-6 h for the iso-conjugates (iso-[211At]SAGMB-5F7, 74.3 ± 2.8%, vs. [211At]SAGMB-5F7, 63.7 ± 0.4% at 2 h) with the opposite behavior observed at 24 h. Peak tumor uptake for iso-[211At]SAGMB-5F7 was 23.4 ± 2.2% ID/g at 4 h, slightly lower than its radioiodinated counterpart, but significantly higher than observed with [211At]SAGMB-5F7. Except in kidneys and lungs, tumor-to-normal organ ratios for iso-[211At]SAGMB-5F7 were greater than 10:1 by 2 h, and significantly higher than those for [211At]SAGMB-5F7. CONCLUSION:These 211At-labeled sdAb conjugates, particularly iso-[211At]SAGMB-5F7, warrant further evaluation for targeted α-particle radiotherapy of HER2-expressing cancers.

journal_name

Nucl Med Biol

journal_title

Nuclear medicine and biology

authors

Choi J,Vaidyanathan G,Koumarianou E,Kang CM,Zalutsky MR

doi

10.1016/j.nucmedbio.2017.09.003

subject

Has Abstract

pub_date

2018-01-01 00:00:00

pages

10-20

eissn

0969-8051

issn

1872-9614

pii

S0969-8051(17)30244-5

journal_volume

56

pub_type

杂志文章

相关文献

NUCLEAR MEDICINE AND BIOLOGY文献大全
  • Inhibition of carnitine-acyl transferase I by oxfenicine studied in vivo with [11C]-labeled fatty acids.

    abstract：METHODS:Anesthetized pigs were studied with [(11)C]-labeled fatty acids (FAs) with carbon chain length ranging from 8 to 16 carbon atoms, during control conditions and during inhibition of carnitine-palmitoyl transferase I (CPT I) with oxfenicine. The myocardial uptake of [(11)C]-FAs from blood was measured together wi...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2005.03.003

    authors： Angsten G,Valind S,Takalo R,Neu H,Meurling S,Långström B

    更新日期：2005-07-01 00:00:00

  • Binding properties of the cerebral alpha4beta2 nicotinic acetylcholine receptor ligand 2-[18F]fluoro-A-85380 to plasma proteins.

    abstract：INTRODUCTION:To determine the availability of nicotinic acetylcholine receptors in different human brain regions using the positron emission tomography (PET) radioligand 2-[18F]fluoro-A-85380 (2-[18F]FA) and invasive approaches for quantification, it is important to correct the arterial input function as well for plasm...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2006.07.012

    authors： Sorger D,Becker GA,Hauber K,Schildan A,Patt M,Birkenmeier G,Otto A,Meyer P,Kluge M,Schliebs R,Sabri O

    更新日期：2006-10-01 00:00:00

  • Radiolabelling and evaluation of a novel sulfoxide as a PET imaging agent for tumor hypoxia.

    abstract：:[¹⁸F]FMISO is the most widely validated PET radiotracer for imaging hypoxic tissue. However, as a result of the pharmacokinetics of [¹⁸F]FMISO a 2h wait between tracer administration and patient scanning is required for optimal image acquisition. In order to develop hypoxia imaging agents with faster kinetics, we have...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2014.03.001

    authors： Laurens E,Yeoh SD,Rigopoulos A,Cao D,Cartwright GA,O'Keefe GJ,Tochon-Danguy HJ,White JM,Scott AM,Ackermann U

    更新日期：2014-05-01 00:00:00

  • Radiosynthesis of [11C]brofaromine, a potential tracer for imaging monoamine oxidase A.

    abstract：:Brofaromine (4-5(-methoxy-7-bromobenzofuranyl)-2-piperidine-HCl) is a potent and selective inhibitor of monoamine oxidase (MAO) A. Two methods for its synthesis and a preliminary positron emission tomography (PET) evaluation in monkey brain are described. The first method, at low carrier concentration of CO2, consiste...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/0969-8051(95)02051-9

    authors： Ametamey SM,Beer HF,Guenther I,Antonini A,Leenders KL,Waldmeier PC,Schubiger PA

    更新日期：1996-04-01 00:00:00

  • Radiochemical synthesis of [123I]2-iodo-lisuride for dopamine D2-receptor studies.

    abstract：:By variation of reaction parameters iodination of 3-(9,10-didehydro-6-methyl-8 alpha-ergolinyl)-1,1-diethylurea (lisuride) was performed with the radiohalogen [123I]iodine (t1/2 = 13.3 h). For comparative experiments and stability studies the beta(-)-emitting radioisotope [131I]iodine (t1/2 = 8.04 d) was also used. Re...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/0969-8051(96)00018-2

    authors： Bier D,Dutschka K,Knust EJ

    更新日期：1996-04-01 00:00:00

  • Comparison of N-[(11)C]methyl-norchloroepibatidine and N-[(11)C]methyl-2-(2-pyridyl)-7-azabicyclo[2.2.1]heptane with N-[(11)C]methyl-epibatidine in small animal PET studies.

    abstract：:Structural variations of the nicotinic acetylcholine receptor radioligand N-[(11)C]methyl-epibatidine were made to form (11)C-labeled N-methyl-norchloroepibatidine (N-methyl-NorchloroEPB) and N-methyl-2-(2-pyridyl)-7-azabicyclo[2.2.1]heptane (N-methyl-2PABH). Radiosyntheses were performed by methylation with high radi...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(00)00080-9

    authors： Spang JE,Patt JT,Westera G,Schubiger PA

    更新日期：2000-04-01 00:00:00

  • High-resolution imaging of brain 5-HT 1B receptors in the rhesus monkey using [11C]P943.

    abstract：:The serotonin 5-HT(1B) receptors regulate the release of serotonin and are involved in various disease states, including depression and schizophrenia. The goal of the study was to evaluate a high affinity and high selectivity antagonist, [(11)C]P943, as a positron emission tomography (PET) tracer for imaging the 5-HT(...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2009.10.007

    authors： Nabulsi N,Huang Y,Weinzimmer D,Ropchan J,Frost JJ,McCarthy T,Carson RE,Ding YS

    更新日期：2010-02-01 00:00:00

  • (E)-[125I]-5-AOIBV: a SPECT radioligand for the vesicular acetylcholine transporter.

    abstract：:The premise that, over the course of Alzheimer's disease (AD), changes in the levels of the vesicular acetylcholine transporter (VAChT) occur in parallel with changes to other cholinergic marker proteins provides the basis for the applicability of benzovesamicol derivatives as radioligands for AD studies by single pho...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2007.07.011

    authors： Emond P,Mavel S,Zea-Ponce Y,Kassiou M,Garreau L,Bodard S,Drossard ML,Chalon S,Guilloteau D

    更新日期：2007-11-01 00:00:00

  • Studies of quality control of 99mTc-labelled macroaggregated albumin--Part 1. Aggregation of non-mercaptalbumin and its conformation.

    abstract：:The aggregative condition of albumin was investigated using bovine serum albumin (BSA) as a model for quality control of 99mTc-macroaggregated albumin (99mTc-MAA). Uniformalized aggregates were obtained from the oxidized non-mercapt-type of BSA by heating. The size of the aggregates was affected by the pH and the type...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/0969-8051(93)90034-r

    authors： Fukuoka M,Kobayashi T,Satoh T,Tanaka A,Kubodera A

    更新日期：1993-07-01 00:00:00

  • True tracers: comparing FDG with glucose and FLT with thymidine.

    abstract：:As PET metabolic imaging becomes routine in clinical practice, there is a tendency to make imaging and data analysis fast and simple, but interpretation of these pictures by visual inspection does not do justice to the power of PET technology. Tissue data and blood data can be analyzed mathematically to provide parame...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章,评审

    doi：10.1016/j.nucmedbio.2005.04.004

    authors： Krohn KA,Mankoff DA,Muzi M,Link JM,Spence AM

    更新日期：2005-10-01 00:00:00

  • 2-[18F]Fluoro-A-85380, an in vivo tracer for the nicotinic acetylcholine receptors.

    abstract：:The in vivo brain regional distribution of 2-[18F]fluoro-A-85380, a novel tracer for positron emission tomographic (PET) studies, followed the regional densities of brain nAChRs reported in the literature. Evidence of binding to nAChRs and high specificity of the binding in vivo was demonstrated by inhibition with nAC...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(98)00031-6

    authors： Horti AG,Scheffel U,Koren AO,Ravert HT,Mathews WB,Musachio JL,Finley PA,London ED,Dannals RF

    更新日期：1998-10-01 00:00:00

  • Biodistribution studies of two 18F-labeled pyridinylphenyl amides as subtype selective radioligands for the dopamine D3 receptor.

    abstract：INTRODUCTION:Dopamine D3 receptors are implicated in various neuropsychiatric diseases, drug abuse and alcoholism, but specific agents for D3 molecular imaging are lacking. We evaluated two in vitro selective fluorine-18-labeled radioligand candidates ([(18)F]5 and [(18)F]6) for positron emission tomography (PET) imagi...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2013.12.014

    authors： Hocke C,Cumming P,Maschauer S,Kuwert T,Gmeiner P,Prante O

    更新日期：2014-03-01 00:00:00

  • A simplified one-pot synthesis of 9-[(3-[18F]fluoro-1-hydroxy-2-propoxy)methyl]guanine([18F]FHPG) and 9-(4-[18F]fluoro-3-hydroxymethylbutyl)guanine ([18F]FHBG) for gene therapy.

    abstract：:9-[(3-[18F]Fluoro-1-hydroxy-2-propoxy)methyl]guanine ([18F]FHPG, 2) has been synthesized by nucleophilic substitution of N(2)-(p-anisyldiphenylmethyl)-9-[[1-(p-anisyldiphenylmethoxy)-3-toluenesulfonyloxy-2-propoxy]methyl]guanine (1) with potassium [18F]fluoride/Kryptofix 2.2.2 followed by deprotection with 1 N HCl and...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(01)00253-0

    authors： Shiue GG,Shiue CY,Lee RL,MacDonald D,Hustinx R,Eck SL,Alavi AA

    更新日期：2001-10-01 00:00:00

  • Synthesis and evaluation of (11)C-labeled (S)-N-[[1-(2-phenylethyl) pyrrolidin-2-yl]methyl]-3-methylthiobenzamide as a PET 5-HT(1A) receptor ligand.

    abstract：:We prepared 5-HT(1A) receptor ligands (S)-N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]-3-[11C]methylthiobenzamide ([11C](S)-PPMMB) (Ki = 4.3 nM) and the less active [(11)C](R)-PPMMB (Ki = 160 nM) by reduction of the disulfide dimer and subsequent [(11)C]methylation of demethyl (S)- and (R)-PPMMB, respectively. Both ra...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(02)00305-0

    authors： Fujio M,Nagata S,Kawamura K,Sugiyama N,Tanaka H,Uno K,Ishiwata K

    更新日期：2002-08-01 00:00:00

  • Heterogeneity of plasma gonadotropins. Consequences on immunological properties of LH.

    abstract：:The pituitary gonadotropins FSH and LH are secreted into blood as dimeric glycoproteins which display a wide heterogeneity when submitted to technique of separation based on electric charge. That supports the assumption of a major role of the carbohydrates moieties as a source of heterogeneity. No clear difference how...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章,评审

    doi：10.1016/0969-8051(94)90058-2

    authors： Roger M,Lalhou N

    更新日期：1994-04-01 00:00:00

  • Kinetic characterization of hexokinase isoenzymes from glioma cells: implications for FDG imaging of human brain tumors.

    abstract：:Quantitative imaging of glucose metabolism of human brain tumors with PET utilizes 2-[(18)F]-fluorodeoxy-D-glucose (FDG) and a conversion factor called the lumped constant (LC), which relates the metabolic rate of FDG to glucose. Since tumors have greater uptake of FDG than would be predicted by the metabolism of nati...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(00)00201-8

    authors： Muzi M,Freeman SD,Burrows RC,Wiseman RW,Link JM,Krohn KA,Graham MM,Spence AM

    更新日期：2001-02-01 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

  • Comparison of trans-1-amino-3-[18F]fluorocyclobutanecarboxylic acid (anti-[18F]FACBC) accumulation in lymph node prostate cancer metastasis and lymphadenitis in rats.

    abstract：INTRODUCTION:Trans-1-amino-3-[(18)F]fluorocyclobutanecarboxylic acid (anti-[(18)F]FACBC) is a positron emission tomography (PET) tracer used to visualize prostate cancer (PCa). In this study, we investigated the differences in anti-[(18)F]FACBC accumulation between metastatic and inflamed lymph node (LN) lesions. METH...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2014.04.004

    authors： Kanagawa M,Doi Y,Oka S,Kobayashi R,Nakata N,Toyama M,Shirakami Y

    更新日期：2014-08-01 00:00:00

  • Difference in brain distributions of carbon 11-labeled 4-hydroxy-2(1H)-quinolones as PET radioligands for the glycine-binding site of the NMDA ion channel.

    abstract：:High-affinity iodine- and ethyl-C-5 substituted analogs of 4-hydroxy-3-(3-[11C]methoxyphenyl)-2(1H)-quinolone ([11C]4HQ) were synthesized as new positron emission tomography radioligands for the glycine-binding sites of the N-methyl-d-aspartate (NMDA) ion channel. Although both radioligands showed high in vitro specif...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2007.10.007

    authors： Fuchigami T,Haradahira T,Fujimoto N,Okauchi T,Maeda J,Suzuki K,Suhara T,Yamamoto F,Sasaki S,Mukai T,Yamaguchi H,Ogawa M,Magata Y,Maeda M

    更新日期：2008-02-01 00:00:00

  • Radiolabelling and PET brain imaging of the α₁-adrenoceptor antagonist Lu AE43936.

    abstract：:Cerebral α₁-adrenoceptors are a common target for many antipsychotic drugs. Thus, access to positron emission tomography (PET) brain imaging of α₁-adrenoceptors could make important contributions to the understanding of psychotic disorders as well as to the pharmacokinetics and occupancy of drugs targeting the α₁-adre...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2012.09.010

    authors： Risgaard R,Ettrup A,Balle T,Dyssegaard A,Hansen HD,Lehel S,Madsen J,Pedersen H,Püschl A,Badolo L,Bang-Andersen B,Knudsen GM,Kristensen JL

    更新日期：2013-01-01 00:00:00

  • [125/123I] 5-Iodo-3-pyridyl ethers. syntheses and binding to neuronal nicotinic acetylcholine receptors.

    abstract：:Three 3-pyridyl ether nicotinic ligands-(S)-5-Iodo-3-[(2-pyrrolidinyl)-methoxy]pyridine (5-iodo-A-85865), (S)-5-Iodo-3-[1-(methyl)-2-pyrrolidinyl-methoxy]pyridine (5-Iodo-A-84543), and (S)-5-iodo-3-[1-methyl-(2-azetidinyl)-methoxy]pyridine (5-iodo-N-Me-A-85380) were labeled with I-125/I-123, and their ability to label...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(01)00258-x

    authors： Fan H,Scheffel UA,Rauseo P,Xiao Y,Dogan AS,Yokoi F,Hilton J,Kellar KJ,Wong DF,Musachio JL

    更新日期：2001-11-01 00:00:00

  • Cardiac lymphatic dynamics after ischemia and reperfusion--experimental model.

    abstract：:ABSTRACT. The aim of the present study was to investigate the lymphatic cardiac circulation in an experimental model of ischemia plus reperfusion in mongrel dogs (Canis familiaris L). As radiotracer we used 0.2-0.25 ml (111 MBq) of 99mTc-Re2S7 colloid (+/-10 microm), injected subcapsullary below the second diagonal of...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(98)00037-7

    authors： Santos AC,de Lima JJ,Botelho MF,Pacheco MF,Sousa P,Bernardo J,Ferreira N,Gonçalves L,Aguiar J,Providência LA,Pauwels EK

    更新日期：1998-10-01 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 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

  • Column-switching HPLC for the analysis of plasma in PET imaging studies.

    abstract：:A column-switch high performance liquid chromatography method for the analysis of 4 mL of plasma is described with six examples of chromatography of [(11)C]-labeled positron-emission tomography imaging agents. Complete extraction of all but the most polar metabolites by the reverse phase capture column is achieved by ...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(00)00125-6

    authors： Hilton J,Yokoi F,Dannals RF,Ravert HT,Szabo Z,Wong DF

    更新日期：2000-08-01 00:00:00

  • Radio-copper-labeled Cu-ATSM: an indicator of quiescent but clonogenic cells under mild hypoxia in a Lewis lung carcinoma model.

    abstract：UNLABELLED:The purpose of this study is to reveal characteristics of (64)Cu-labeled diacetyl-bis(N(4)-methylthiosemicarbazone) ([(64)Cu]Cu-ATSM) during cell proliferation and hypoxia by autoradiography imaging and immunohistochemical staining. METHODS:The intratumoral distributions of [(64)Cu]Cu-ATSM and [(18)F]-2-flu...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2009.01.016

    authors： Oh M,Tanaka T,Kobayashi M,Furukawa T,Mori T,Kudo T,Fujieda S,Fujibayashi Y

    更新日期：2009-05-01 00:00:00

  • Clinical acceptance of a molecular imaging agent: a long march with [99mTc]TRODAT.

    abstract：:In the past 10 years, significant progress has been made in using a technetium-99m dopamine transporter imaging agent, [99mTc]TRODAT, for routine clinical studies. Developing a molecular imaging agent from bench to the bedside is more than a simple scientific venture. Currently, Taiwan is the only place where [99mTc]T...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章,评审

    doi：10.1016/j.nucmedbio.2007.03.010

    authors： Kung HF,Kung MP,Wey SP,Lin KJ,Yen TC

    更新日期：2007-10-01 00:00:00

  • [¹⁸F]Altanserin and small animal PET: impact of multidrug efflux transporters on ligand brain uptake and subsequent quantification of 5-HT₂A receptor densities in the rat brain.

    abstract：INTRODUCTION:The selective 5-hydroxytryptamine type 2a receptor (5-HT(2A)R) radiotracer [(18)F]altanserin is a promising ligand for in vivo brain imaging in rodents. However, [(18)F]altanserin is a substrate of P-glycoprotein (P-gp) in rats. Its applicability might therefore be constrained by both a differential expres...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2013.09.001

    authors： Kroll T,Elmenhorst D,Matusch A,Celik AA,Wedekind F,Weisshaupt A,Beer S,Bauer A

    更新日期：2014-01-01 00:00:00

  • Preclinical evaluation of (99m)Tc labeled chondroitin sulfate for monitoring of cartilage degeneration in osteoarthritis.

    abstract：PURPOSE:In previous in-vitro and ex-vivo studies we proved the specific uptake of (99m)Tc radiolabeled chondroitin sulfate (CS) in human articular cartilage. As a logical next step for the clinical use for imaging osteoarthritis we investigated in-vivo uptake of (99m)TcCS in dogs. PROCEDURES:The radiolabeling of CS Co...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2016.02.009

    authors： Sobal G,Velusamy K,Kosik S,Menzel J,Hacker M,Pagitz M

    更新日期：2016-06-01 00:00:00

  • PET imaging with ⁸⁹Zr: from radiochemistry to the clinic.

    abstract：:The advent of antibody-based cancer therapeutics has led to the concomitant rise in the development of companion diagnostics for these therapies, particularly nuclear imaging agents. A number of radioisotopes have been employed for antibody-based PET and SPECT imaging, notably ⁶⁴Cu, ¹²⁴I, ¹¹¹In, and (99m)Tc; in recent...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章,评审

    doi：10.1016/j.nucmedbio.2012.08.004

    authors： Deri MA,Zeglis BM,Francesconi LC,Lewis JS

    更新日期：2013-01-01 00:00:00