Abstract：
:The Cu(I)-assisted aromatic halogen exchange proved useful for preparation of macroscopic amounts of 2-iodophenyl-metyrapone as well as for the n.c.a. radioiodinated analogue. Semi-preparative HPLC-isolation provided the compound with high purity for use as chromatographic standard and for the determination of the inhibition constant of the 2-iodo-analogue. The non-isotopic exchange led to a high specific activity (> 5000 GBq/mumol) of 2-[123I]iodophenyl-metyrapone. A reaction in acetic acid at elevated temperatures proved superior to an exchange in aqueous solution with in-situ reduction of Cu2+. Even without Cu+ high radiochemical yields of > 80% were obtained, while addition of Cu+ provided the radiotracer with 95% radiochemical yield within 5 minutes in acetic acid.
journal_name
Nucl Med Bioljournal_title
Nuclear medicine and biologyauthors
Schirbel A,Coenen HHdoi
10.1016/0969-8051(95)02033-0subject
Has Abstractpub_date
1995-11-01 00:00:00pages
1075-9issue
8eissn
0969-8051issn
1872-9614pii
0969805195020330journal_volume
22pub_type
杂志文章abstract：OBJECTIVES:To compare the radiolabeling performance, stability, and practical efficacy of the chelators CHX-A″-DTPA and H4octapa with the therapeutic radiometal (90)Y. METHODS:The bifunctional chelators p-SCN-Bn-H4octapa and p-SCN-Bn-CHX-A″-DTPA were conjugated to the HER2-targeting antibody trastuzumab. The resulting...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2016.06.004
更新日期：2016-09-01 00:00:00
abstract：:Using positron emission tomography (PET) and nitric oxide radiolabeled with nitrogen-13 (half-life 9.97 min) we probed the distribution and kinetics of inhaled nitric oxide in anesthetized dogs. The washout of this gas after inhalation was much slower than that observed for [13N]nitrogen gas, demonstrating its uptake ...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/0969-8051(96)00072-8
更新日期：1996-08-01 00:00:00
abstract：INTRODUCTION:Sepantronium bromide (YM155) is an antitumor drug in development and is a first-in-class chemical entity, which is a survivin suppressant. We developed a radiosynthesis of [(11)C]YM155 to non-invasively evaluate its tissue and tumor distribution in mice bearing human prostate tumor xenografts. METHODS:Met...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2012.10.002
更新日期：2013-02-01 00:00:00
abstract：:The properties of two prospective positron emission tomography (PET) ligands for the delta-opioid receptor, N1'-fluoroethyl-naltrindole (BU97001) and N1'-fluoroethyl-(14-formylamino)-naltrindole (BU97018) were investigated. Both were antagonists in the mouse vas deferens, and showed high affinity and selectivity, 1.81...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(02)00300-1
更新日期：2002-05-01 00:00:00
abstract：:Copper offers a unique selection of radioisotopes ((60)Cu, (61)Cu, (62)Cu, (64)Cu, and (67)Cu) with half-lives ranging from 9.8 min to 61.9 h suitable for imaging and/or radiotherapy. In peptide/antibody targeted radiotherapy one of the most studied chelating agents for copper, 1,4,8,11-tetraazacyclotetradecane-1,4,8,...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章,评审
doi：10.1016/s0969-8051(01)00287-6
更新日期：2002-01-01 00:00:00
abstract：PURPOSE:This study aimed to assess the striatal [(18)F]FE-PE2I binding and the immunohistochemical stain of tyrosine hydroxylase (TH) in the striatum, and to evaluate the effects of therapeutic drugs on [(18)F]FE-PE2I binding. METHODS:Dynamic PET/CT of [(18)F]FE-PE2I was performed in Parkinson's disease (PD) rat model...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2015.11.002
更新日期：2016-02-01 00:00:00
abstract：:The pharmacokinetics and internal radionuclide therapy of intraperitoneally administrated (188)Re-N,N-bis(2-mercaptoethyl)-N',N'-diethylethylenediamine (BMEDA)-labeled pegylated liposomal doxorubicin ((188)Re-DXR-liposome) were investigated in the C26 murine colon carcinoma ascites mouse model. After intraperitoneal a...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2008.09.005
更新日期：2008-11-01 00:00:00
abstract：:The in vitro metabolism of 1-(4-[(18)F]fluoromethylbenzyl)-4-phenylpiperazine ([(18)F]1) and 1-(4-[(18)F]fluorobenzyl)-4-phenylpiperazine ([(18)F]2) was investigated using mouse liver S9 fraction. Results were compared to those of in vivo metabolism using mouse blood and bone and to in vitro metabolism using mouse liv...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2005.12.002
更新日期：2006-02-01 00:00:00
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
更新日期：2010-02-01 00:00:00
abstract：:An in vivo estimation of the newly synthesized MAO-A specific inhibitor, [125I]-labeled N-[3(2,4-dichloro-6-iodophenoxy)propyl]-N-methyl-2- propynylamine ([125I]-iodoclorgyline), was performed. Retention of the radioactivity of this radioligand was observed in the brain from 1 h post-injection. Pretreatments with clor...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/0969-8051(94)00105-s
更新日期：1995-02-01 00:00:00
abstract：:Macrophages are a major inflammatory cell type involved in the development and progression of many important chronic inflammatory diseases. We previously found that apolipoprotein E-deficient (Apoe(-/-)) mice with the C57BL/6 (B6) background develop type 2 diabetes mellitus (T2DM) and accelerated atherosclerosis when ...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2014.12.001
更新日期：2015-04-01 00:00:00
abstract：INTRODUCTION:The functions of I₂-imidazoline receptors (I₂Rs) are unknown, but evidence exists for their involvement in various neuropsychiatric disorders. Although a few positron emission tomography (PET) I₂R ligands have been developed, of which [(11)C]FTIMD and [(11)C]BU99008 were evaluated as PET I₂R imaging ligand...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2014.12.014
更新日期：2015-04-01 00:00:00
abstract：INTRODUCTION:Therapeutic application of intravenous administered (IV) human bone marrow-derived mesenchymal stem cells (ahMSCs) appears to have as main drawback the massive retention of cells in the lung parenchyma, questioning the suitability of this via of administration. Intraarticular administration (IAR) could be ...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2016.12.003
更新日期：2017-03-01 00:00:00
abstract：INTRODUCTION:Rodent models are extensively used to assess the biochemical and physiological changes associated with aging. They play a major role in the development of therapies for age-related pathologies such as Parkinson's disease. To validate the usefulness of these animal models in aging or age-related disease res...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2014.12.020
更新日期：2015-04-01 00:00:00
abstract：:An iodinated analog of PK11195, 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)isoquinoline-3-carboxamide , a specific antagonist of the peripheral-type benzodiazepine receptor (omega 3), has been synthesized in three steps with an overall chemical yield of 40%. Both [123I]- and [125I]-Iodo-PK11195 have been synthesize...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/0969-8051(95)02007-1
更新日期：1996-01-01 00:00:00
abstract：INTRODUCTION:Noninvasive imaging of small animals to measure biodistributions and pharmacokinetics of radiolabeled agents is increasingly seen as an effective alternative to external counting of tissues obtained by sacrifice and dissection. However, we have observed important disagreements in measuring the accumulation...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2011.02.004
更新日期：2011-08-01 00:00:00
abstract：:A positron-emitter labeled radioligand for the glycine-binding site of the N-methyl-D-aspartate (NMDA) receptor, [(11)C]L-703,717, was examined for its ability to penetrate the brain in animals by simultaneous use with drugs having high-affinity separate binding sites on human serum albumin. [(11)C]L-703,717 has poor ...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(00)00096-2
更新日期：2000-05-01 00:00:00
abstract：:With [11C]raclopride,[11C]nemonapride and [11C]N-methylspiperone, degeneration of dopamine D2-like receptors in the unilaterally quinolinic acid-lesioned rats was evaluated by positron emission tomography (PET) and ex vivo and in vitro autoradiography. PET showed a decreased uptake of [11C]raclopride in the lesioned s...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(01)00307-9
更新日期：2002-04-01 00:00:00
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
更新日期：1995-08-01 00:00:00
abstract：:Technetium-99m-modified polylysine (MPL) is a mild and efficient method for cell labeling that is easily applicable to human lymphocytes. 99mTc-MPL uptake is maximal in 40 min at room temperature. Cell labeling efficiency (from 60 to 80%) increases with rising concentrations of cells and labeling agent. In vitro stabi...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/0969-8051(95)02011-x
更新日期：1996-01-01 00:00:00
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
更新日期：2013-02-01 00:00:00
abstract：:In vivo pharmacokinetic and brain binding characteristics of [18F]RP 62203, a selective high-affinity serotonergic 5-HT2A receptor antagonist, were assessed in the rat following intravenous injection of trace amount of the radioligand. The radioactive distribution profile observed in the brain 60 min after injection w...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/0969-8051(95)02008-x
更新日期：1996-02-01 00:00:00
abstract：INTRODUCTION:The remarkable stability of the 89Zr-DOTA complex has been shown in recent literature. The formation of this complex appears to require 89Zr-chloride as the complexation precursor rather than the more conventional 89Zr-oxalate. In this work we present a method for the direct isolation of 89Zr-chloride from...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2018.06.003
更新日期：2018-01-01 00:00:00
abstract：:To investigate possible changes in somatostatin receptor expression during treatment with high dose lanreotide, eight patients with neuroendocrine tumors were investigated by [(111)In-DTPA-D-Phe1]-octreotide scintigraphy before and during treatment. The spleen-to-background ratio decreased in all patients, whereas tum...
journal_title：Nuclear medicine and biology
pub_type： 临床试验,杂志文章
doi：10.1016/s0969-8051(99)00059-1
更新日期：1999-11-01 00:00:00
abstract：INTRODUCTION:This study investigated radiolabeled bacteriophages for specific detection of infection through gamma imaging. Previously, a (99m)Tc-labeled M13 phage demonstrated specific binding for its host Escherichia coli in vitro and in mice through imaging. METHODS:This study was extended to phages P22, E79, VD-13...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2008.02.011
更新日期：2008-05-01 00:00:00
abstract：:The pyridopyrimidinones are a potent class of inhibitors of c-Abl kinase and Bcr-Abl kinase, the causative fusion protein in chronic myelogenous leukemia and Src family kinases. A novel method for routine, high-yield no-carrier-added synthesis of [(124)I]-, [(125)I]- and [(131)I]-6-(2,6-dichlorophenyl)-2-(4-iodophenyl...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2005.01.008
更新日期：2005-05-01 00:00:00
abstract：OBJECTIVES:Radiolabeled amino acids have proven utility for imaging brain tumors in humans, particularly those that target system L amino acid transport. We have prepared the novel phenylalanine analogue, (FMePhe, 9), as part of an effort to develop new system L tracers that can be prepared in high radiochemical yield ...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2012.12.013
更新日期：2013-05-01 00:00:00
abstract：:A new tetrahydrazido-germanium (GeTH) ligand was synthesized, characterized and complexed with 99mTc. The negatively charged 99mTc-chelate was shown to form in high yields at neutral pH in the absence of other reducing agents and exhibits high in vitro and in vivo stability. ...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/0969-8051(94)90184-8
更新日期：1994-11-01 00:00:00
abstract：INTRODUCTION:Nuclear and optical imaging are complementary in many aspects and there would be many advantages when optical imaging probes are prepared using radionuclides rather than classic fluorophores, and when nuclear and optical dual images are obtained using single imaging probe. METHODS:The luminescence intensi...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2010.09.003
更新日期：2011-04-01 00:00:00
abstract：UNLABELLED:(18)F-9-fluoropropyl-(+)-dihydrotetrabenazine ((18)F-AV-133) is a novel positron emission tomography tracer for imaging the vesicular monoamine transporter II in dopaminergic neuron degeneration, which might be indicative for Parkinson's disease (PD) and other parkinsonism. Studies were performed to optimize...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2011.05.010
更新日期：2011-11-01 00:00:00
