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). In order to be useful for immuno-PET chelators are required to both stabilize the radionuclide in terms of coordination chemistry and to facilitate the covalent attachment to the targeting vector. Different chelators were evaluated for this purpose in terms of radiolabelling efficiency and stability of the radiolabelled Nb(V) complex and in order to determine the most suitable candidate for conjugation to a biologically relevant targeting vector. For the purpose of studying the complexation properties the niobium radioisotope (95)Nb was used as an analogue of (90)Nb, by virtue of its longer half-life (35 days) and lower cost (reactor-based production). Acyclic and cyclic chelators were investigated, with desferroxamine [Df: (N'-{5-[acetyl(hydroxy)amino]pentyl}-N-[5-({4-[(5-aminopentyl) (hydroxy)amino]-4-oxobutanoyl} amino)pentyl]-N-hydroxysuccinamide)] emerging as the best candidate. Greater than 99% radiolabelling was achieved at room temperature over a wide pH range. The (95)Nb-Df complex is sufficiently stable for immuno-PET (<7% degradation over 7 days in vitro). As a proof-of-principle, a Df conjugate featuring a well-established targeting vector, (D)-Phe(1)-octreotide, was evaluated. The fast labelling kinetics of the unconjugated chelator (Df) were retained for Df-succinyl-(D)Phe(1)-octreotide (Df-OC), with>90% labelling after 1h at room temperature over the pH range 5-7. Stability studies, performed in vitro in serum at physiological temperature (37 °C), revealed that 87 ± 2% of the radiolabelled molecule remained intact after 7 days. Competition studies with relevant metal ions (zirconium((IV)), gallium((III)) and iron((III))) have been performed with Df-OC to gain insight to the relative stability [Nb-Df]-OC complex to transmetallation. At equimolar metal ion concentrations the [Nb-Df]-OC complex showed the greatest overall stability. The favourable radiolabelling characteristics of Df-OC and its stability indicate that Df is a potentially very useful chelator for the development of radiopharmaceuticals for (90)Nb-PET.
journal_name
Nucl Med Bioljournal_title
Nuclear medicine and biologyauthors
Radchenko V,Busse S,Roesch Fdoi
10.1016/j.nucmedbio.2014.06.006subject
Has Abstractpub_date
2014-10-01 00:00:00pages
721-7issue
9eissn
0969-8051issn
1872-9614pii
S0969-8051(14)00438-7journal_volume
41pub_type
杂志文章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::Copper-64-labeled monoclonal antibodies (mAbs) have previously demonstrated unexpectedly effective tumor control in rodent models of cancer at relatively low tumor-absorbed radiation doses. This property has been associated with delivery platforms resulting in cellular internalization. The purpose of the present studi...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2005.05.006
更新日期:2005-11-01 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::We report a single pass gas phase route to [11C]CH3I based on production of I from I2 at elevated temperature. I abstracts H from CH4 to yield CH3, which reacts with I2 to form CH3I. A fiber optic spectrometer was used to measure the I2 vapor concentration. [11C]CH3I yield increased with I2 concentration until excessi...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/s0969-8051(96)00181-3
更新日期:1997-01-01 00:00:00
abstract::The discovery of neuroendocrine differentiation in hormone-refractory prostatic adenocarcinoma has opened a potentially new therapeutic approach in this group of patients with a poor prognosis and few effective therapy modalities. Based on previous findings of increased uptake of 11C-5-hydroxytryptophan (11C-5-HTP) in...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/s0969-8051(97)00064-4
更新日期:1997-05-01 00:00:00
abstract:INTRODUCTION:Hypoxia plays a negative role in the clinical management of cancer. Detection of hypoxic status of a cancer is important for selecting patients for hypoxia directed therapy. Though [(18)F]fluoromisonidazole ([(18)F]FMISO), a PET radiopharmaceutical, is presently being used in the clinic for the detection o...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2014.04.103
更新日期:2014-08-01 00:00:00
abstract::Myocellular kinetics of 201Tl, 99mTc-MIBI, 99mTc-tetrofosmin and 99mTc-furifosmin were investigated using retrogradely-perfused guinea-pig hearts. Relative retention decreased in the order 99mTc-MIBI ==> 99mTc-tetrofosmin ==> 99mTc-furifosmin. 201Tl and 99mTc-MIBI exhibited bi- (t1,t2), 99mTc-tetrofosmin and 99mTc-fur...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/s0969-8051(01)00288-8
更新日期:2002-02-01 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:OBJECTIVE:Pretargeting is the concept that combines optimal delivery of the antibody and rapid capture and elimination of the radioactivity. In this study, we evaluated the potential of antibody pretargeting to enable the tumor-targeting (212)Pb for in vivo generation of (212)Bi for alpha particle radiotherapy. METHOD...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2005.06.009
更新日期:2005-10-01 00:00:00
abstract:INTRODUCTION:Renal uptake of Tc-99m-MG3 involves organic anion transporter (OAT). Treatment with drugs showing OAT affinity might interfere with renal uptake of Tc-99m-MAG3, leading to misinterpretation in Tc-99m-MAG3. This study was conducted to discuss a possible drug interference with Tc-99m-MAG3 diagnosis on OAT si...
journal_title:Nuclear medicine and biology
pub_type: 临床试验,杂志文章
doi:10.1016/j.nucmedbio.2013.03.006
更新日期:2013-07-01 00:00:00
abstract::In developing radioiodinated agents for pancreatic and brain tumor imaging by single photon emission tomography (SPET), we prepared p-amino-3-[123I]iodo-l-phenylalanine (IAPA), p-[123I]iodo-l-phenylalanine (IPA), L-8-[123I]iodo-1,2,3,4-tetrahydro-7-hydroxyisoquinoline-3-carboxylic acid (ITIC) and L-3-[123I]iodo-alpha-...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/s0969-8051(00)00176-1
更新日期:2001-01-01 00:00:00
abstract::To fully exploit the potential of positron emission tomography (PET) imaging to assess drug distribution and pharmacokinetics in the central nervous system, the contribution of radiometabolites to the PET signal has to be determined for correct interpretation of data. However, radiosynthesis and extensive study of rad...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2020.08.001
更新日期:2020-01-01 00:00:00
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
更新日期:2005-10-01 00:00:00
abstract:OBJECTIVE:Herpes simplex virus type 1 thymidine kinase (HSV1-tk) gene in combination with radiolabeled nucleoside substrates is the most widely used reporter system. This study characterized 1-(2'-deoxy-2'-[(18)F]fluoro-β-D-arabinofuranosyl)-5-iodocytosine ((18)F-FIAC) as a new potential positron emission tomography (P...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2011.04.003
更新日期:2011-10-01 00:00:00
abstract::Rhenium-186 (Re-186) hydroxyethylidene diphosphonate (HEDP) has been shown to localize in metastatic foci within bone in a manner similar to Tc-99m bone-seeking agents. Usually, in the preparation of diagnostic Tc-99m radiopharmaceuticals, the concentration of Tc is at trace level (10(-8) M). However, large amounts of...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/s0969-8051(99)00007-4
更新日期:1999-05-01 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::The gastrin releasing peptide (GRP) receptor is becoming an increasingly attractive target for development of new radiolabeled peptides with diagnostic and therapeutic potential. The attractiveness of the GRP receptor as a target is based upon the functional expression of GRP receptors in several tumors of neuroendocr...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章,评审
doi:10.1016/s0969-8051(03)00116-1
更新日期:2003-11-01 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::[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
更新日期:2014-05-01 00:00:00
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
更新日期:2001-11-01 00:00:00
abstract::In the last few years click chemistry reactions, and in particular copper-catalyzed cycloadditions have been used extensively for the preparation of new bioconjugated molecules such as (18)F-radiolabeled radiopharmaceuticals for positron emission tomography (PET). This study is focused on the synthesis of the Siemens ...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2013.04.003
更新日期:2013-07-01 00:00:00
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 inh...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/0969-8051(95)02033-0
更新日期:1995-11-01 00:00:00
abstract:INTRODUCTION:Human epidermal growth factor receptor type 2 (HER2) overexpression supports proliferation of androgen-independent prostate cancer (PC). Radionuclide molecular imaging of HER2 expression in disseminated PC would aid in the selection of patients who are likely responders to HER2 targeting therapy. In this s...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2011.04.005
更新日期:2011-11-01 00:00:00
abstract:INTRODUCTION:Dysregulation of the hepatocyte growth factor (HGF)/MET pathway has been implicated in various cancers. Rilotumumab is an investigational, fully human monoclonal antibody that binds and neutralizes HGF. The purpose of this study was to evaluate the efficacy of rilotumumab in a U-87 MG mouse xenograft tumor...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2013.01.004
更新日期:2013-05-01 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:The commercially available 68Ge/68Ga generators are generally used in clinical context in conjunction with automated or semi-automated modules for the syntheses of 68Ga radiopharmaceuticals. It is desirable to develop strategies for the formulation of 68Ga-radiopharmaceuticals without use of such expensive...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2016.11.006
更新日期:2017-03-01 00:00:00
abstract::Matrix metalloproteinase-2 (MMP-2) is a key enzyme involved in tumor invasiveness. (2R)-2- [4-(6-[(18)F]Fluorohex-1-ynyl)-benzenesulfonylamino]-3-methylbutyric acid ([(18)F]SAV03), a new fluorine-18 labeled MMP-2 inhibitor developed for tumor imaging with PET, was biologically evaluated using in vivo tumor model. Enzy...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/s0969-8051(02)00393-1
更新日期:2003-02-01 00:00:00
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
更新日期:1999-07-01 00:00:00
abstract::Because more and more PET centres are using small proton cyclotrons there is a renewed interest in methods for the production of electrophilic 18F by proton irradiation of [18O]O2. A method for the routine production of clinically useful quantities of [18F]F2 having a specific activity of 35 Ci/mmol has been developed...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/0969-8051(94)e0064-p
更新日期:1995-01-01 00:00:00
abstract:UNLABELLED:The purpose of this study was to compare the diagnostic value of positron emission tomography (PET) using [(18)F]-fluorodeoxyglucose ((18)F-FDG) and O-(2-[(18)F]fluoroethyl)-l-tyrosine ((18)F-FET) in patients with brain lesions suspicious of cerebral gliomas. METHODS:Fifty-two patients with suspicion of cer...
journal_title:Nuclear medicine and biology
pub_type: 临床试验,杂志文章
doi:10.1016/j.nucmedbio.2009.05.005
更新日期:2009-10-01 00:00:00