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 plasma protein binding (PPB) of the radioligand as for radiolabeled metabolites accumulating in blood. This study deals with some aspects of PPB of 2-[18F]FA. METHODS:Patients with different neurological disorders (n=72), such as Parkinson's disease, Alzheimer's disease and multiple sclerosis, and a group of healthy volunteers (n=15) subjected for PET imaging were analyzed for their PPB level of 2-[18F]FA using ultrafiltration. Protein gel electrophoresis of plasma samples was performed to identify the binding protein of 2-[18F]FA. The dependency of PPB on time and on free ligand concentration was analyzed to obtain the binding parameters Bmax and Kd. RESULTS:Albumin was identified to be the binding protein of 2-[18F]FA. PPB of 2-[18F]FA was low at 17+/-4% and did not show significant differences between the groups of patients. Corresponding to this, a narrow range of plasma albumin of 0.62+/-0.05 mM was observed. Bmax was determined as twice the albumin concentration, which indicates two binding sites for 2-[18F]FA on the protein. No time dependence of the PPB could be observed. By relating PPB to Bmax, an average Kd value of 6.0+/-1.5 mM was obtained. CONCLUSION:This study shows the dependency of PPB of 2-[18F]FA on human albumin plasma concentration. An equation utilizing Bmax and Kd to easily estimate PPB is presented.
journal_name
Nucl Med Bioljournal_title
Nuclear medicine and biologyauthors
Sorger D,Becker GA,Hauber K,Schildan A,Patt M,Birkenmeier G,Otto A,Meyer P,Kluge M,Schliebs R,Sabri Odoi
10.1016/j.nucmedbio.2006.07.012subject
Has Abstractpub_date
2006-10-01 00:00:00pages
899-906issue
7eissn
0969-8051issn
1872-9614pii
S0969-8051(06)00151-Xjournal_volume
33pub_type
杂志文章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
abstract：INTRODUCTION:This paper proposes liposomes as a potential new tool for radioimmunotherapy in solid tumours with a two step targeting system. Tumour pretargeting is obtained by using a monoclonal bispecific antibody (BsmAb, anti CEA x anti-DTPA-In) and pegylated liposomes containing lipid-hapten (DSPE-DTPA-In or DSPE-PE...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2013.12.012
更新日期：2014-05-01 00:00:00
abstract：:Among the ways to deliver comparatively large amounts of boron to cells in vitro for boron neutron capture studies is the linkage of a boronated macromolecule such as polylysine to an antibody. In order to reduce interference with immunoreactivity, boronated polylysine (BPL) was linked to oligosaccharide moieties on t...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(01)00297-9
更新日期：2002-02-01 00:00:00
abstract：INTRODUCTION:The identification of sentinel lymph nodes (SLNs) is important in deciding the resection range during surgery. 99mTc-labeled mannosylated human serum albumin ([99mTc]Tc-MSA) is a radiopharmaceutical developed for SLN detection by targeting macrophages. Evans blue (EB) is a blue dye binding strongly to albu...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2020.02.002
更新日期：2020-01-01 00:00:00
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
更新日期：2013-01-01 00:00:00
abstract：INTRODUCTION:After its intravenous injection, [18F]fluorocholine is oxidized by choline-oxidase into its main plasma metabolite, [18F]fluorobetaine. If PET kinetic modeling quantification of [18F]fluorocholine uptake is intended, the plasma input time-activity-curve of the parent tracer must be obtained, i.e., the frac...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2019.08.003
更新日期：2019-01-01 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：:A radioiodinated ligand, (R)-N-methyl-(2-[(125)I]iodo-phenoxy)-3-phenylpropylamine, [(125)I]2-INXT, targeting norepinephrine transporters (NET), was successfully prepared. A no-carrier-added product, [(125)I]2-INXT, displayed a saturable binding with a high affinity (K(d)=0.06 nM) in the homogenates prepared from rat ...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2004.03.001
更新日期：2004-07-01 00:00:00
abstract：INTRODUCTION:Gonadotropin releasing hormone (GnRH) receptor is overexpressed in many human tumors. Previously we developed a 18F-labelled GnRH peptide. Although the GnRH-targeted PET probe can be clearly visualized by microPET imaging in a PC-3 xenograft model, clinical applications of the probe have been limited by co...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2020.02.004
更新日期：2020-01-01 00:00:00
abstract：INTRODUCTION:HDAC6, a structural and functional distinct member of the HDAC-family, shows great promise as a target to treat several cancers and neurodegenerative diseases. Several clinical trials are evaluating HDAC6 inhibitors in solid tumours and haematological malignancies, but so far no HDAC6 inhibitor has receive...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2019.05.004
更新日期：2019-01-01 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：:Antagonists of neurokinin receptors such as CP-643,051 are presently under investigation as potential antidepressants, but little is known about the brain uptake and distribution of these agents. We developed a method for the efficient N-[11C]methylation of CP-122,721, yielding the NK1 antagonist N-[11C]methyl CP-643,...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2004.03.005
更新日期：2004-08-01 00:00:00
abstract：INTRODUCTION:Positron emission tomography (PET) is extensively used in clinical oncology for tumor detection. This study aimed to explore the application of the radiotracers [18F]fluorodeoxyglucose ([18F]FDG), 3'-deoxy-3'- [18F]fluorothymidine ([18F]FLT), and [18F]fluoromisonidazole ([18F]FMISO) in the diagnosis and mo...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2019.07.004
更新日期：2019-01-01 00:00:00
abstract：:Radiolabeled lipiodol has been used for targeting liver cancer. We developed a lipiodol solution of (188)Re-TDD (2,2,9,9-tetramethyl-4,7-diaza-1,10-decanedithiol) and investigated its feasibility for the treatment of liver cancer. The lipiodol solution of (188)Re-TDD was well-retained in the lipiodol phase in vitro. A...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(00)00208-0
更新日期：2001-02-01 00:00:00
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
更新日期：2007-10-01 00:00:00
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
更新日期：2009-05-01 00:00:00
abstract：INTRODUCTION:VEGF receptors play a key role in angiogenesis and are important targets for several approved and many experimental drugs. Imaging of VEGF receptor expression in malignant tumors would provide important information, which can influence patient management. The aim of this study was the development of an eas...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2010.02.001
更新日期：2010-05-01 00:00:00
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
更新日期：2017-02-01 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：OBJECTIVES:Serotonin transporters (SERT) play an important role in controlling serotonin concentration in the synaptic cleft and in managing postsynaptic signal transduction. Inhibitors of SERT binding are well known as selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine, sertraline, paroxetine, and esci...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2018.06.008
更新日期：2018-11-01 00:00:00
abstract：:Synthesis and preliminary biological evaluation of 9-(4-[18F]-fluoro-3-hydroxymethylbutyl)-guanine ([18F]FHBG) is reported. 9-(4-Hydroxy-3-hydroxymethylbutyl)-guanine (penciclovir) 4 was converted to 9-[N2, O-bis-(methoxytrityl)-3-(tosylmethybutyl)]guanine 7 by treatment with methoxytrityl chloride followed by tosylat...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(97)00160-1
更新日期：1998-04-01 00:00:00
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
更新日期：1993-07-01 00:00:00
abstract：UNLABELLED:The radiolabelled bombesin analogue AMBA shows high potential for diagnosis and treatment of prostate and breast cancer, but the influence of different chelators, which differ in terms of radiochemical reactivity and stability, have not been explored so far. In order to find the best suitable chelator for la...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2013.08.010
更新日期：2014-01-01 00:00:00
abstract：:A simple method is described for affinity purification of radiolabeled antibodies using glutaraldehyde-fixed tumor target cells. The cell-bound antibody fraction is removed from the cells by an acid wash and then immediately subjected to buffer-exchange chromatography. The method was applied to the D3 murine monoclona...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/0969-8051(93)90053-w
更新日期：1993-04-01 00:00:00
abstract：:Applications of oligodeoxynucleotides to modulate gene expression have been the subject of much recent research. We have sought to develop a method to permanently inactivate a gene, or potentially kill cells containing abnormal genes. In this report, we show that a DNA intercalator conjugated to a triplex-forming olig...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/0969-8051(96)00034-0
更新日期：1996-05-01 00:00:00
abstract：:A consensus has emerged that early imaging (within 20 min post-injection [p.i.] of sestamibi) has the highest diagnostic yield. Tc-99m-sestamibi uptake has been associated with P-glycoprotein-mediated multi-drug resistance (MDR), tumor vascularization, invasiveness, and cell proliferation. The aim of this study was to...
journal_title：Nuclear medicine and biology
pub_type： 临床试验,杂志文章
doi：10.1016/s0969-8051(98)00026-2
更新日期：1998-08-01 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：: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
更新日期：1996-04-01 00:00:00
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
更新日期：2009-11-01 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
