Abstract：
INTRODUCTION:The in vitro and in vivo behavior of the radiolabeled monoclonal antibody MORAb-003 was investigated as a prelude to a clinical trial. METHODS:The cellular retention of 111In- and 131I-labeled MORAb-003 was investigated using IGROV1 and SW620 cells. Biodistribution studies in tumor-bearing mice were performed with the more favorable agent. RESULTS:Five 1,4,7,10-tetraazacyclododecane-N,N',N",N'"-tetraacetic acid (DOTA) molecules were conjugated to MORAb-003 with no apparent loss of immunoreactivity. Radiolabeled MORAb-003 had a high affinity for the folate receptor alpha (FRA) expressed by both IGROV1 and SW620 cells and was found to bind to around 8 x 10(5) and 7 x 10(5) sites/cell, respectively. Both cancer cell lines were found to internalize both 131I- and 111In-labeled MORAb-003, but 111In was retained and 131I was released as iodide. In athymic mice, 111In-DOTA-MORAb-003 was cleared from the blood with a single exponential biological clearance rate of 110 h. The uptake in SW620 tumors was 32+/-5%ID/g after 4 days. The clearance rate of activity from normal organs such as liver, kidney and spleen was similar to the blood clearance and was 5.36%ID/g, 4.03%ID/g and 4.36%ID/g at 1 day postinjection and 2.14%ID/g, 1.65%ID/g and 3.74%ID/g after 8 days, respectively. In a pilot clinical study, the biodistribution and tumor targeting of 111In-MORAb-003 was assessed in three patients undergoing treatment with cold MORAb-003. CONCLUSION:MORAb-003 is an attractive antibody for radioimmunoscintigraphy and possibly radioimmunotherapy of FRA-expressing cancers in addition to its potential direct therapeutic effects.
journal_name
Nucl Med Bioljournal_title
Nuclear medicine and biologyauthors
Smith-Jones PM,Pandit-Taskar N,Cao W,O'Donoghue J,Philips MD,Carrasquillo J,Konner JA,Old LJ,Larson SMdoi
10.1016/j.nucmedbio.2007.12.008subject
Has Abstractpub_date
2008-04-01 00:00:00pages
343-51issue
3eissn
0969-8051issn
1872-9614pii
S0969-8051(08)00006-1journal_volume
35pub_type
杂志文章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
更新日期：2000-08-01 00:00:00
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
更新日期：2001-11-01 00:00:00
abstract：:The herpes simplex virus type 1 thymidine kinase (HSV1-TK) reporter system is being used to directly and indirectly monitor therapeutic gene expression, immune cell trafficking and protein-protein interactions in various living animals. However, the issues of HSV1-TK enzyme stability in living cells and whether this r...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2006.04.001
更新日期：2006-07-01 00:00:00
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
更新日期：2012-07-01 00:00:00
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
更新日期：1994-04-01 00:00:00
abstract：:Cholinergic system in the central nervous system is involved in the memory function. Thus, because the dysfunction of cholinergic system that project to the cerebral cortex from nucleus basalis of Meynert (nbM) would be implicated in the memory function deficits in Alzheimer's disease (AD), evaluating cholinergic func...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2005.06.013
更新日期：2006-02-01 00:00:00
abstract：INTRODUCTION:The tricyclic indole compound, [(18)F]GE-180 has been previously identified as a promising positron emission tomography (PET) imaging agent of the translocator protein (TSPO) with the potential to aid in the diagnosis, prognosis and therapy monitoring of degenerative neuroinflammatory conditions such as mu...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2015.05.004
更新日期：2015-09-01 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：:We investigated sigma(1) and dopamine D(2) receptor occupancy in mouse brain after a single injection of haloperidol, nemonapride, or spiperone using [(11)C]SA4503 and [(11)C]raclopride, respectively. Co-injection of the three compounds significantly blocked the uptake of each radioligand. Six hours later, only halope...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(03)00003-9
更新日期：2003-05-01 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：: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：:NCQ 115 ((+)-(R)-5-bromo-N-((1-(4-fluorobenzyl)-2-pyrrolidinyl)methyl)-2, 3-dimethoxybenzamide) is a selective dopamine D-2 receptor antagonist. NCQ 115 has a fluorine in a synthetically suitable position in the parent compound and was therefore suggested as a potential 18F-labelled radioligand for positron emission t...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/0969-8051(94)90028-0
更新日期：1994-05-01 00:00:00
abstract：:188Re-perrhenate has been reported effective in preventing restenosis after percutaneous transluminal coronary angioplasty. However, if the balloon ruptures, 188Re-perrhenate is released into the circulation, causing high radiation dosing to the thyroid and stomach. In this study, we evaluated the effects of perchlora...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(99)00079-7
更新日期：2000-01-01 00:00:00
abstract：:In connection with pretargeting, an amine-derivatized morpholino phosphorodiamidate oligomer (NH(2)-cMORF) was conjugated conventionally with p-isothiocyanate benzyl-DTPA (p-SCN-Bn-DTPA). However, after (111)In radiolabeling, unexpected label instability was observed. To understand this instability, the NH(2)-cMORF an...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2010.08.008
更新日期：2011-02-01 00:00:00
abstract：UNLABELLED:Gastrin-releasing peptide receptors (GRPr) are a member of the bombesin (BBN) receptor family. GRPr are expressed in high numbers on specific human cancers, including human prostate cancer. Therefore, copper-64 ((64)Cu) radiolabeled BBN(7-14)NH(2) conjugates could have potential for diagnosis of human prosta...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2010.04.016
更新日期：2010-10-01 00:00:00
abstract：INTRODUCTION:Nanoscale perfluorocarbon (PFC) droplets have been used to create imaging agents and drug delivery vehicles. However, development and characterization of new formulations of PFC droplets are hindered because of the lack of simple methods for quantitative and sensitive assessment of whole body tissue distri...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2017.07.001
更新日期：2017-11-01 00:00:00
abstract：:Metabolic studies of (111)In-DTPA-labeled polypeptides and peptides showed that the radiolabeled (poly)peptides generated (111)In-DTPA-adducts of amino acid that possess long residence times in the lysosomal compartment of the tissues where (poly)peptides accumulated. However, a recent study suggested that metal-chela...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(01)00207-4
更新日期：2001-05-01 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：:Indium-111 labeled, Trastuzumab-Doxorubicin Conjugated, and APTES-PEG coated magnetic nanoparticles were designed for tumor targeting, drug delivery, controlled drug release, and dual-modal tumor imaging. Superparamagnetic iron oxide nanoparticles (SPIONs) were synthesized by thermal decomposition method to obtain nar...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2014.09.007
更新日期：2015-02-01 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：:Dual probe microdialysis was employed in intact rat brain to investigate the effect of intrastriatal perfusion with selective dopamine D1 and D2 receptor agonists and with c-fos antisense oligonucleotide on (a) local GABA release in the striatum; (b) the internal segment of the globus pallidus and the substantia nigra...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(98)00066-3
更新日期：1998-11-01 00:00:00
abstract：:meta-[18F]Fluorobenzylguanidine ([18F]MFBG) and para-[18F]fluorobenzylguanidine ([18F]PFBG) were synthesized in three steps beginning with a fluoro for nitro exchange reaction on 3- and 4-nitrobenzonitrile, respectively. Overall radiochemical yields were 10-15% for [18F]MFBG and 50-55% for [18F]PFBG in a total synthes...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/0969-8051(94)90135-x
更新日期：1994-01-01 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：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：: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
更新日期：2009-08-01 00:00:00
abstract：INTRODUCTION:Carbonic anhydrase (CA) IX is a transmembrane protein overexpressed in many frequently occurring tumors associated with tumor hypoxia. Sulfonamides and their bioisosteres are known to inhibit CA IX activity. In this study, 4-(2-aminoethyl)benzenesulfonamide was conjugated to a tridentate ligand, N-2-picoly...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2010.02.006
更新日期：2010-07-01 00:00:00
abstract：INTRODUCTION:The alpha-7 nicotinic acetylcholine receptor (α7 nAChR) is key in brain communication and has been implicated in the pathophysiology of diseases of the central nervous system. A positron-emitting radioligand targeting the α7 nAChR would enable better understanding of a variety of neuropsychiatric illnesses...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2013.04.005
更新日期：2013-08-01 00:00:00
abstract：INTRODUCTION:The dopamine D4 receptor (D4R) has attracted considerable attention as potential target for the treatment of a broad range of central nervous system disorders. Although many efforts have been made to improve the performance of putative radioligand candidates, there is still a lack of D4R selective tracers ...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2020.07.004
更新日期：2020-07-16 00:00:00
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
更新日期：1996-04-01 00:00:00
abstract：BACKGROUND:The radiolabeled amino acid O-(2-(18)F-fluoroethyl)-L-tyrosine (FET) and thymidine analogue 3'-deoxy-3'-(18)F-fluorothymidine (FLT) are widely used for positron emission tomography (PET) brain tumor imaging; however, comparative studies are scarce. The aim of this study therefore was to compare FLT and FET P...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2015.12.002
更新日期：2016-03-01 00:00:00
