A useful EGFR-TK ligand for tumor diagnosis with SPECT: development of radioiodinated 6-(3-morpholinopropoxy)-7-ethoxy-4-(3'-iodophenoxy)quinazoline.


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.


Ann Nucl Med


Hirata M,Kanai Y,Naka S,Yoshimoto M,Kagawa S,Matsumuro K,Katsuma H,Yamaguchi H,Magata Y,Ohmomo Y




Has Abstract


2013-06-01 00:00:00












  • The prognostic role of end-of-treatment FDG-PET/CT in diffuse large B cell lymphoma: a pilot study application of neural networks to predict time-to-event.

    abstract:PURPOSE:To evaluate the prognostic role of end-of-treatment (EoT) FDG-PET/CT parameters in diffuse large B cell lymphoma (DLBCL), and then to explore a pilot application of Neural Networks (NN) in predicting time-to-relapse. METHODS:For conventional survival analysis, parameters as Deauville score (DS) and quantitativ...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Annunziata S,Pelliccioni A,Hohaus S,Maiolo E,Cuccaro A,Giordano A

    更新日期:2021-01-01 00:00:00

  • Impaired coronary microvascular function in diabetics.

    abstract::Global and regional myocardial uptake was determined with technetium-99m tetrofosmin and a 4 hour exercise (370 MBq i.v.) and rest (740 MBq i.v.) protocol, in 24 patients with non-insulin dependent diabetes mellitus and in 22 control subjects. The purpose of this study was to evaluate impaired coronary microvascular f...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Tsujimoto G

    更新日期:2000-06-01 00:00:00

  • FDG-PET of patients with suspected renal failure: standardized uptake values in normal tissues.

    abstract:OBJECTIVE:This study aims to clarify the effect of renal function on 2-[(18)F] fluoro-2-deoxy-D-glucose positron emission tomography (FDG-PET) imaging and determine the clinical significance of renal function in this setting. We compared FDG distribution between normal volunteers and patients with suspected renal failu...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Minamimoto R,Takahashi N,Inoue T

    更新日期:2007-06-01 00:00:00

  • Assessment of lung toxicity caused by bleomycin and amiodarone by Tc-99m HMPAO lung scintigraphy in rats.

    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


    authors: Gumuser G,Vural K,Varol T,Parlak Y,Tuglu I,Topal G,Sayit E

    更新日期:2013-08-01 00:00:00

  • Preoperative F-18 fluorocholine PET/CT for the detection of hyperfunctioning parathyroid glands in patients with secondary or tertiary hyperparathyroidism: comparison with Tc-99m sestamibi scan and neck ultrasound.

    abstract:OBJECTIVES:Currently, neck ultrasound is the preferred preoperative imaging in patients with secondary/tertiary hyperparathyroidism, and the use of Tc-99m sestamibi scan is limited in these patients. We conducted this study to compare the diagnostic utilities of F-18 fluorocholine PET/CT, Tc-99m sestamibi scintigraphy,...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Chen YH,Chen HT,Lee MC,Liu SH,Wang LY,Lue KH,Chan SC

    更新日期:2020-08-01 00:00:00

  • FDG-PET imaging in duodenal cancer.

    abstract::F-18 fluorodeoxyglucose positron emission tomography (FDG-PET) imaging is a useful modality in the detection of various tumors, including colon cancer and gastric cancer. We evaluated a patient with duodenal cancer with multiple metastases including brain metastases using FDG-PET imaging. It revealed multiple tumor up...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Watanabe N,Hayashi S,Kato H,Shimizu M,Kamisaki Y,Noguchi K,Kishida M,Matsunari I,Hisada K,Seto H

    更新日期:2004-06-01 00:00:00

  • Unsuccessful tracer injection in radionuclide cisternography revisited.

    abstract::Since cerebrospinal fluid (CSF) leakage is highlighted as a cause of persistent headache, radionuclide cisternography has been increasingly performed in Japan to confirm the disorder, although the limited ability of the examination should be recognized. We present 3 cases in which failure of a tracer injection was str...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Horikoshi T,Asari Y,Watanabe A,Uchida M,Umeda T,Kolzumi H,Kinouchi H

    更新日期:2006-05-01 00:00:00

  • Assessment of ampulla (Takotsubo) cardiomyopathy with coronary angiography, two-dimensional echocardiography and 99mTc-tetrofosmin myocardial single photon emission computed tomography.

    abstract:UNLABELLED:We studied the causative mechanism of ampulla (Takotsubo) cardiomyopathy. METHODS:We examined 7 patients with ampulla cardiomyopathy by means of coronary angiography, two-dimensional echocardiography and 99Tc-tetrofosmin myocardial SPECT at the time of emergency admission (acute phase), at 3 to 5 days after...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Ito K,Sugihara H,Kawasaki T,Yuba T,Doue T,Tanabe T,Adachi Y,Katoh S,Azuma A,Nakagawa M

    更新日期:2001-08-01 00:00:00

  • Clinical usefulness of positron emission tomography with fluorine-18-fluorodeoxyglucose in the diagnosis of liver tumors.

    abstract::We studied various liver tumors by positron emission tomography with fluorine-18 fluorodeoxyglucose (FDG-PET) to examine the diagnostic usefulness of this technique. We also examined the relation between findings on FDG-PET and the characteristics of hepatocellular carcinoma. FDG-PET was performed in 78 patients with ...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Iwata Y,Shiomi S,Sasaki N,Jomura H,Nishiguchi S,Seki S,Kawabe J,Ochi H

    更新日期:2000-04-01 00:00:00

  • Clinical need for both scintigraphy with technetium-99m GSA and per-rectal portal scintigraphy in some patients with chronic liver disease.

    abstract::Scintigraphy with 99mTc-diethylenetriaminepentaacetate with galactosyl human serum albumin (99mTc-GSA) and per-rectal portal scintigraphy are useful for evaluating hepatic functional reserve and portal circulation, respectively. We did the procedures simultaneously in some patients to examine the relationship between ...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Shiomi S,Iwata Y,Sasaki N,Kurooka H,Tamori A,Habu D,Takeda T,Nishiguchi S,Kuroki T,Ochi H

    更新日期:1999-08-01 00:00:00

  • New semiquantitative assessment of 123I-FP-CIT by an anatomical standardization method.

    abstract:UNLABELLED:We evaluated a new semiquantitative procedure to more easily and objectively estimate the striatal uptake of 123I-FP-CIT in patients with Parkinsonian syndrome (PS) and essential tremor (ET), using an anatomical standardization method, the Neurostat. METHODS:Eleven patients with PS and 8 with ET were examin...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Takada S,Yoshimura M,Shindo H,Saito K,Koizumi K,Utsumi H,Abe K

    更新日期:2006-08-01 00:00:00

  • Usefulness of cerebral blood flow (CBF) measurements to predict the functional outcome for rehabilitation in patients with cerebrovascular disease (CVD).

    abstract:PURPOSE:The objectives of this study were to (1) elucidate the relationship between the mean CBF in the whole brain (Av.mCBF) before rehabilitation of CVD patients and the BI score before and after rehabilitation, (2) determine whether the efficacy of rehabilitation can be predicted by measurement of the Av.mCBF, and (...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Tamamoto F,Sumi Y,Nakanishi A,Okayasu K,Maehara T,Katayama H

    更新日期:2000-02-01 00:00:00

  • Metastatic calcification: accumulation of a bone tracer during dynamic data acquisition.

    abstract::Metastatic calcification is often detected by bone scintigraphy. We recently saw metastatic calcification in the stomach and kidneys of a patient on continuous ambulatory peritoneal dialysis. Tc-99m HMDP accumulation into both organs was noted even in the first frame of dynamic data acquisition of 4 min/frame, suggest...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Kinuya S,Taki J,Fujioka M,Michigishi T,Tonami N

    更新日期:1996-11-01 00:00:00

  • Prognostic role of baseline 18F-FDG PET/CT metabolic parameters in mantle cell lymphoma.

    abstract:OBJECTIVE:Mantle cell lymphoma (MCL) is an aggressive lymphoma sub-type with poor prognosis and high 18F-FDG avidity at PET/CT; nowadays, no validated criteria for PET/CT in treatment response evaluation and prediction of outcome are present. The aim of study was to investigate whether the metabolic PET/CT features may...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Albano D,Bosio G,Bianchetti N,Pagani C,Re A,Tucci A,Giubbini R,Bertagna F

    更新日期:2019-07-01 00:00:00

  • Cost-effective initial assessment strategies for thyroid nodules in iodine-adequate areas.

    abstract:OBJECTIVE:In the initial assessment of thyroid nodules, thyrotropin (TSH) has very low sensitivity for assessing functional thyroid nodules (FTNs). The false negativity in FTNs and the false positivity in non-FTNs misinterpreted by TSH will raise unnecessary assessment costs. Therefore, the aim of this study is to expl...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Cai H,Qiao Y,Huang X,Sun M,Luo Q,Yuan X,Yang Y,Mao W,Lv Z

    更新日期:2017-01-01 00:00:00

  • The reproducibility of deep-inspiration breath-hold (18)F-FDG PET/CT technique in diagnosing various cancers affected by respiratory motion.

    abstract:BACKGROUND:The deep-inspiration breath-hold PET/CT (DIBH PET/CT) technique improves the limitations of diagnosing a lesion located in an area influenced by respiratory motion that results in spatial misregistrations caused by respiration between PET and CT. However, its reproducibility with regard to calculating the ma...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Nagamachi S,Wakamatsu H,Kiyohara S,Fujita S,Futami S,Arita H,Tamura S,Kawai K

    更新日期:2010-04-01 00:00:00

  • Similar T/N ratio between 18F-FBPA diagnostic and BPA therapeutic dosages for boron neutron capture therapy in orthotropic tongue cancer model.

    abstract:OBJECTIVE:The tumor-to-normal tissue (T/N) boron ratio is determined in a patient prior to boron neutron capture therapy (BNCT) using 4-borono-2-18F-fluoro-L-phenylalanine (18F-FBPA) positron emission tomography (PET). The T/N ratio is used as a reference parameter to calculate BNCT dose and to evaluate treatment effec...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Lin YC,Chou FI,Yang BH,Chang CW,Chen YW,Hwang JJ

    更新日期:2020-01-01 00:00:00

  • The use of quantitative scintigraphy in the measurement of portal-systemic shunting in rats.

    abstract::Portal-systemic shunting was studied in 54 portal hypertensive rats both in vivo and in vitro using radioactive microspheres. The animals underwent partial portal vein ligation around needles of varying diameter to produce a wide range of shunting. Two to four weeks later, quantitative lung-liver scintigraphic and who...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Stauber RE,Mochizuki T,Van Thiel DH,Tauxe WN

    更新日期:1992-11-01 00:00:00

  • 18F-FDG PET/CT in visceral leishmaniasis: uptake patterns in the context of a multiannual outbreak in Northern Italy.

    abstract:OBJECTIVES:Visceral leishmaniasis (VL) is the most severe manifestation of the infection caused by the protozoan Leishmania, recently on increase in Italy and Spain. The aim of the study was to describe FDG uptake patterns in VL patients (pts) who underwent 18F-FDG PET/CT. METHODS:A retrospective monocentric study of ...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Zanoni L,Varani S,Attard L,Morigi JJ,Vanino E,Ortalli M,Fonti C,Viale P,Re MC,Fanti S,Ambrosini V

    更新日期:2019-09-01 00:00:00

  • Bone metabolic markers as gauges of metastasis to bone: a review.

    abstract::Currently, imaging techniques are the leading methods used to diagnose of metastasis to bone. However, these techniques are expensive, expose patients to toxic and radioactive compounds, and monitor response to treatment poorly; these drawbacks have prompted the search for alternative screening methods. Therefore, bon...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章,评审


    authors: Koizumi M,Ogata E

    更新日期:2002-05-01 00:00:00

  • A systematic review of the prognostic value of texture analysis in 18F-FDG PET in lung cancer.

    abstract:OBJECTIVE:The aim of this study was to perform a systematic review of the prognostic value of texture parameters derived by 18F-fluorodeoxyglucose positron emission tomography (18F-FDG PET) in patients with lung cancer. METHODS:PubMed and EMBASE databases were searched up to March 12, 2018, for original articles invol...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章,meta分析,评审


    authors: Han S,Woo S,Suh CH,Kim YJ,Oh JS,Lee JJ

    更新日期:2018-11-01 00:00:00

  • Evaluation of the bubble point test of a 0.22-μm membrane filter used for the sterilizing filtration of PET radiopharmaceuticals.

    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


    authors: Hayashi K,Douhara K,Kashino G

    更新日期:2014-07-01 00:00:00

  • 18F-FDG and 11C-choline uptake in proliferating tumor cells is dependent on the cell cycle in vitro.

    abstract:OBJECTIVE:Among different PET tracers, 18F-fludeoxyglucose (FDG) and 11C-choline are known to have a high tumor uptake correlated with a high mitotic index of tumor cells. Thus, the uptake of 18F-FDG and 11C-choline may be dependent on the cell cycle. In the present study, we examined the uptake of 18F-FDG and 11C-chol...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Roppongi M,Izumisawa M,Terasaki K,Muraki Y,Shozushima M

    更新日期:2019-04-01 00:00:00

  • Peritoneal tuberculosis with elevated serum CA125 mimicking peritoneal carcinomatosis on F-18 FDG-PET/CT.

    abstract::18F-fluorodeoxyglucose positron emission tomography (F-18 FDG-PET) plays an important role in differentiating benign from malignant tumors. However, some false-positive findings, such as tuberculosis, may occur. We report a case referred for F-18 FDG whole-body PET computed tomography (PET/CT) scan owing to an elevate...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Chen CJ,Yao WJ,Chou CY,Chiu NT,Lee BF,Wu PS

    更新日期:2008-07-01 00:00:00

  • The role of adrenocortical scintigraphy in the evaluation of unilateral incidentally discovered adrenal and juxtaadrenal masses.

    abstract::We reviewed the findings of adrenocortical scintigraphy with 131I-6-beta-iodomethyl-19-norcholesterol (NCL-6-131I) of 39 patients to clarify its role in the evaluation of unilateral adrenal or juxtaadrenal masses incidentally discovered by CT, ultrasonography or plain radiography. Twenty-seven benign adrenal masses sh...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Nakajo M,Nakabeppu Y,Yonekura R,Iwashita S,Goto T

    更新日期:1993-08-01 00:00:00

  • The role of technetium-99m-HMPAO-labeled WBC scintigraphy in the diagnosis of orbital cellulitis.

    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


    authors: Sayit E,Söylev M,Capa G,Durak I,Ada E,Yilmaz M,Durak H

    更新日期:2001-02-01 00:00:00

  • Feasibility and kinetic characteristics of (68)Ga-NOTA-RGD PET for in vivo atherosclerosis imaging.

    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


    authors: Paeng JC,Lee YS,Lee JS,Jeong JM,Kim KB,Chung JK,Lee DS

    更新日期:2013-11-01 00:00:00

  • Demonstration of systemic lymphnodes by bone scintigraphy in amyloidosis.

    abstract::We report a case of primary amyloidosis with calcification of systemic lymphnodes which were demonstrated as positives by bone scintigraphy. Positive sites delineated by bone scintigraphy would seem likely to reflect avid calcification of amyloid deposits. The discovery of positive systemic lymphnodes by bone scintigr...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Itoh K,Baba Y,Taneichi K

    更新日期:1992-05-01 00:00:00

  • Usefulness of the Chang attenuation correction method with use of a CT-based μ map by FBP reconstruction in (201)Tl SPECT-MPI.

    abstract:OBJECTIVE:Attenuation correction (AC) on nuclear images of non-uniform domains is generally performed by a change of the computed tomography (CT) values to μ values, which are then inserted as components into the detection probability of iterative reconstruction techniques (OS-EM Iterative AC). We established an AC tec...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Nakamura Y,Tomiguchi S

    更新日期:2015-06-01 00:00:00

  • Double-phase (131)I whole body scan and (131)I SPECT-CT images in patients with differentiated thyroid cancer: their effectiveness for accurate identification.

    abstract:OBJECTIVE:This study aims to determine whether a (131)I double-phase whole body scan (WBS) and SPECT-CT images have added value over a single-phase WBS image in identifying benign and malignant lesions in patients with well-differentiated thyroid cancer (DTC) at their first radioactive iodine (RAI) treatment. METHODS:...

    journal_title:Annals of nuclear medicine

    pub_type: 杂志文章


    authors: Wakabayashi H,Nakajima K,Fukuoka M,Inaki A,Nakamura A,Kayano D,Kinuya S

    更新日期:2011-11-01 00:00:00