Abstract:
OBJECTIVE:Epidermal growth factor receptor tyrosine kinase (EGFR-TK) represents an attractive target for tumor diagnosis agents. Previously, radioiodinated 4-(3-iodophenoxy)-6,7-diethoxyquinazoline (PHY) was reported to possess good characteristics as a tumor imaging agent. We have explored the feasibility of developing tumor diagnosis ligands superior to radioiodinated PHY. METHODS:New phenoxyquinazoline derivatives were designed with various side chains introduced to the 6th position of PHY. The IC50 values of the new derivatives to interrupt EGFR-TK phosphorylation were evaluated and compared to well-known EGFR-TK inhibitors. Tumor uptake studies of the new (125)I-labeled derivatives were conducted with A431 tumor-bearing mice. Selectivity and binding characteristics were analyzed by in vitro blocking studies and a binding assay. Furthermore, SPECT/CT scans were performed using A431 tumor-bearing mice. RESULTS:Six quinazoline derivatives were designed and synthesized, and among these, 6a-d were found to have relatively high EGFR-TK inhibitory potency. In tumor uptake studies, [(125)I]6a ([(125)I]PYK) was found to have the highest tumor uptake and longest retention in tumors. In contrast, [(125)I]PYK was rapidly cleared from peripheral tissues, resulting in a high tumor-to-tissue ratio 24 h after injection. Moreover, the EGFR-TK selectivity of [(125)I]PYK was confirmed by pretreatment experiments with specific EGFR-TK inhibitors. Furthermore, [(125)I]PYK provided clear SPECT images of tumors. CONCLUSIONS:Radioiodinated PYK, one of the newly synthesized quinazoline derivatives, was found to be a desirable ligand for EGFR-TK SPECT imaging. [(125)I]PYK showed high tumor accumulation and selective EGFR-TK binding and also succeeded in delivering high contrast imaging of tumors. These favorable characteristics of [(125)I]PYK suggest that the (123)I-labeled counterpart, [(123)I]PYK, would have great potential for diagnostic SPECT tumor imaging.
journal_name
Ann Nucl Medjournal_title
Annals of nuclear medicineauthors
Hirata M,Kanai Y,Naka S,Yoshimoto M,Kagawa S,Matsumuro K,Katsuma H,Yamaguchi H,Magata Y,Ohmomo Ydoi
10.1007/s12149-013-0703-ysubject
Has Abstractpub_date
2013-06-01 00:00:00pages
431-43issue
5eissn
0914-7187issn
1864-6433journal_volume
27pub_type
杂志文章abstract:AIM:The aim of the study was to compare the kinetic analysis of 18F-labeled choline (FCH) uptake with static analysis and clinicopathological parameters in patients with newly diagnosed prostate cancer (PC). MATERIALS AND METHODS:Sixty-one patients were included. PSA was performed few days before FCH PET/CT. Gleason s...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-018-1246-z
更新日期:2018-05-01 00:00:00
abstract::123I-BMIPP (beta-methyl-iodophenyl pentadecanoic acid) has shown unique properties for potential use in assessing myocardial metabolism. Previous basic and clinical studies demonstrated that the disturbances of myocardial metabolism precede the occurrence of myocardial perfusion abnormalities by using 201Tl in hypertr...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/BF03165056
更新日期:1996-02-01 00:00:00
abstract:OBJECTIVE:The purpose of this study was to evaluate the usefulness of 18F-fluorodeoxyglucose (FDG) positron emission tomography (PET) in differentiating pulmonary artery sarcoma from pulmonary embolism. MATERIALS AND METHODS:We evaluated three patients with pulmonary artery sarcoma and 10 patients with proximal pulmon...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-009-0292-y
更新日期:2009-09-01 00:00:00
abstract::We report a case of myocardial stunning after acute myocardial infarction. In the hyperacute phase of myocardial infarction, the patient's coronary arteries showed normal features on coronary angiography during extensive ST-segment elevation observed on a standard 12-lead electrocardiogram and extensive akinesis obser...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/BF03165021
更新日期:1994-05-01 00:00:00
abstract::Bacterial orbital cellulitis is an infection of the soft tissues behind the orbital septum. Cellulitis is seen as a poorly defined area of increased CT density or T2 signal intensity within the fat. There is an amorphous enhancement following contrast infusion. Radiolabeled leukocytes or granulocytes are now establish...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/BF03012129
更新日期:2001-02-01 00:00:00
abstract::Positron emission tomography (PET) imaging is in common use preoperatively to clinically evaluate patients who present with central nervous system mass lesions. The usefulness of PET is also recognized as a method to detect intracranial tumorous lesions. A number of papers reportthat some inflammatory processes also s...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/BF02988258
更新日期:2003-02-01 00:00:00
abstract:BACKGROUND:Aortic knob width on chest radiography represents the extent of aortic dialation and tortuosity of the aortic arch. We tested the hypothesis that aortic knob width reflected left ventricular (LV) diastolic function assessed by gated myocardial perfusion single photon emission computed tomography (SPECT) in p...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-017-1150-y
更新日期:2017-04-01 00:00:00
abstract:UNLABELLED:To determine the utility of the myocardial tracer Tc-99m-tetrofosmin in the examination of patients with left bundle branch block (LBBB) and to investigate Tc-99m-tetrofosmin uptake and retention in the myocardium, early and delayed Tc-99m-tetrofosmin SPECT was performed in 10 patients having LBBB without co...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/BF03164914
更新日期:1998-10-01 00:00:00
abstract:OBJECTIVE:Pre-clinical studies with gallium-68 zoledronate ([68Ga]Ga-DOTAZOL) have proposed it to be a potent bisphosphonate for PET/CT diagnosis of bone diseases and diagnostic counterpart to [177Lu]Lu-DOTAZOL and [225Ac]Ac-DOTAZOL. This study aims to be the first human biodistribution and dosimetric analysis of [68Ga...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-019-01348-7
更新日期:2019-06-01 00:00:00
abstract::Physiological functions (e.g., cerebral blood flow, glucose metabolism, and neuroreceptor binding) can be investigated as parameters estimated by kinetic modeling using dynamic positron emission tomography (PET) images. Imaging of these physiological parameters, called parametric imaging, can locate the regional distr...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章,评审
doi:10.1007/s12149-007-0044-9
更新日期:2007-09-01 00:00:00
abstract:OBJECTIVE:We developed a bubble point test kit and investigated the bubble point test of a 0.22-μm membrane filter used for the sterilizing filtration of [(18)F]FDG, [(11)C]MET and [(11)C]PIB. The bubble point test of the Millex-GS vented filter was often difficult due to air leakage from the vented portion of this fil...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-014-0830-0
更新日期:2014-07-01 00:00:00
abstract:AIM:Computer-aided diagnosis (CAD) software for bone scintigrams have recently been introduced as a clinical quality assurance tool. The purpose of this study was to compare the diagnostic accuracy of two CAD systems, one based on a European and one on a Japanese training database, in a group of bone scans from Japanes...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-012-0620-5
更新日期:2012-10-01 00:00:00
abstract:OBJECTIVE:Metabolic tumor burden (MTB) incorporates the advantages of the existing indices: the metabolic volume of the lesion calculated by size-dependent thresholding on positron emission tomography-computed tomography (PET-CT) along with its aggressiveness as determined by standardized uptake value (SUV). This study...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-011-0539-2
更新日期:2012-01-01 00:00:00
abstract:OBJECTIVE:We digested anti-MUC1 monoclonal antibody PR81 to produce F(ab')₂ fragments. A comparison was performed between the two radiolabeled PR81 and F(ab')₂ fragments for breast tumor imaging in a mouse model. METHODS:The optimum conditions for pepsin digestion of PR81 were investigated in terms of enzymes: antibod...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-010-0434-2
更新日期:2011-02-01 00:00:00
abstract:OBJECTIVE:Estimation of myocardial blood flow (MBF) and coronary flow reserve (CFR) by SPECT myocardial perfusion imaging (MPI) remains challenging. Our aim was to approximate MBF and CFR by quantifying the absolute Tc-99m tetrofosmin retention in the myocardium via gated-SPECT/CT MPI. METHODS:Tracer retention was cal...
journal_title:Annals of nuclear medicine
pub_type: 临床试验,杂志文章
doi:10.1007/s12149-015-0982-6
更新日期:2015-08-01 00:00:00
abstract:UNLABELLED:We propose a new method to quantify regional myocardial blood flow (rMBF) by continuous infusion of Tc-99m MIBI and dynamic SPECT. METHODS:Five patients with old myocardial infarction were studied. During continuous infusion of MIBI (approximately 740 MBq) with a syringe pump in 10 min, dynamic SPECT scan w...
journal_title:Annals of nuclear medicine
pub_type: 临床试验,杂志文章
doi:10.1007/BF03165431
更新日期:1999-02-01 00:00:00
abstract:OBJECTIVE:Accurate and validated methods for estimating regional PET image noise are helpful for optimizing image processing. The bootstrap is a data-based simulation method for statistical inference, which can be used to estimate the PET image noise without repeated measurements. The aim of this study was to experimen...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-013-0782-9
更新日期:2014-02-01 00:00:00
abstract::Using the fuzzy set theory, a method was developed for analyzing the extent and severity of ischemia by comparing the exercise and delayed SPECT images with Thallium-201. For each short axial image (slice) for exercise and delayed study, a defect probability matrix (DPM) is created so that it shows the severity of isc...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/BF03164947
更新日期:1988-11-01 00:00:00
abstract:OBJECTIVE:Estimation of nonlinear micro-parameters is a computationally demanding and fairly challenging process, since it involves the use of rather slow iterative nonlinear fitting algorithms and it often results in very noisy voxel-wise parametric maps. Direct reconstruction algorithms can provide parametric maps wi...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-014-0881-2
更新日期:2014-11-01 00:00:00
abstract:OBJECTIVE:In this study, the feasibility and kinetic characteristics of the (68)Ga-NOTA-RGD, a recently developed RGD peptide agent, were investigated for atherosclerosis imaging in comparison with (18)FDG. METHODS:ApoE(-/-) mice were fed a high-fat diet for more than 20 weeks. To evaluate the feasibility, tissue upta...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-013-0757-x
更新日期:2013-11-01 00:00:00
abstract:UNLABELLED:The purpose of this study is to determine the subcellular distribution of thallium (SDTl) by electron microscopy and a newly designed fixation method that makes insoluble grains of Tl visible. METHODS:To obtain the high dose necessary for electron microscopic visualization, we employed TlCl instead of 201Tl...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/BF03165296
更新日期:1997-11-01 00:00:00
abstract:OBJECTIVE:To investigate the correlation between the F-18 FDG uptake in the normal testis as assessed by PET-CT and patient age in a pediatric study population. METHODS:The study population consisted of 22 subjects aged between 9 and 17 years. For these subjects 42 PET-CT scans were available for analysis. The testis ...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-009-0308-7
更新日期:2009-11-01 00:00:00
abstract::Tl-201 SPECT and Tc-99m-Human serum albumin (HSA) multigated radionuclide ventriculography were performed on 11 patients with progressive muscular dystrophy (Becker type 2, Fukuyama type 2, Limb-girdle type 7) to evaluate myocardial involvement. Hypoperfusion was detected in 8 patients on Tl-201 SPECT. Decreases in bo...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/BF03164989
更新日期:1994-02-01 00:00:00
abstract:AIM:The purpose of the study was to determine the lung toxicity caused by amiodarone (AD) and bleomycin (BLM) in rats, by means of Tc-99m HMPAO lung scintigraphy. METHODS:Thirty albino rats were randomly divided into five groups. After AD or BLM was dissolved with isotonic saline (SF), a 0.5 ml solution was applied to...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-013-0722-8
更新日期:2013-08-01 00:00:00
abstract:OBJECTIVE:123I-metaiodobenzylguanidine (MIBG) myocardial scintigraphy is currently used to evaluate cardiac sympathetic nerve function, but MIBG also has the capacity to evaluate dilated cardiomyopathy (DCM) severity and therapeutic effectiveness. In this study, we administered beta-blockers to a DCM hamster model and ...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/BF02984974
更新日期:2003-12-01 00:00:00
abstract:OBJECTIVE:The aim of this study was to evaluate the left ventricular (LV) functional parameters calculated using quantitative electrocardiography (ECG)-gated myocardial perfusion single photon emission computed tomography (QGS). In addition to LV systolic parameters, diastolic parameters were compared with those by ult...
journal_title:Annals of nuclear medicine
pub_type: 临床试验,杂志文章
doi:10.1007/BF02985571
更新日期:2005-09-01 00:00:00
abstract:OBJECTIVE:The potential of positron emission tomography/computed tomography using 62Cu-diacetyl-bis (N4-methylthiosemicarbazone) (62Cu-ATSM PET/CT), which was originally developed as a hypoxic tracer, to predict therapeutic resistance and prognosis has been reported in various cancers. Our purpose was to investigate pr...
journal_title:Annals of nuclear medicine
pub_type: 临床试验,杂志文章
doi:10.1007/s12149-018-1241-4
更新日期:2018-05-01 00:00:00
abstract::We report FDG PET of two cases of cold abscess due to Mycobacterium tuberculosis. Case 1 had colon cancer; FDG PET showed high FDG uptake in the colon lesion and low uptake in the inguinal lesion. The latter was a tuberculous cold abscess confirmed by CT/MRI and biopsy. Case 2 received radiotherapy for lung cancer and...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/BF02985581
更新日期:2005-09-01 00:00:00
abstract:OBJECTIVE:In high-risk patients with left bundle-branch block (LBBB), functional but not perfusion parameters yield incremental prognostic information. The aim of our study was to evaluate the prognostic value of gated single photon emission computed tomography (SPECT) in low-intermediate risk LBBB patients. METHODS:O...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-012-0613-4
更新日期:2012-08-01 00:00:00
abstract::We conducted a study of rCBF in the primary visual cortex of visually impaired subjects who have not been subjected to external stimulation for a long period, by means of 123I-IMP SPECT and MRI. The four subjects had lost their sight due to brain tumors (n = 2), glaucoma (n = 1) and trauma (n = 1). 123I-IMP SPECT show...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/BF03164976
更新日期:1995-05-01 00:00:00