Abstract:
OBJECTIVE:4-Benzyl-1-(3-iodobenzylsulfonyl)piperidine, 4-B-IBSP, has shown high-binding affinity to both sigma (σ) receptors in our previous work. In current study, radiolabeling and preclinical evaluation of 4-benzyl-1-(3-[125I]-iodobenzylsulfonyl)piperidine, 4-B-[125I]IBSP, in human ductal breast carcinoma (T47D) cells and in breast adenocarcinoma-bearing BALB/c mice are described. METHODS:Radioiodination of this new σ ligand was performed by a palladium-catalyzed stannylation approach followed by oxidative iododestannylation reaction using Iodo-Gen. Competition-binding assays for binding of 4-B-[125I]IBSP to guinea pig brain membranes and to T47D cells were performed with known σ ligands. The selectivity and binding characteristics (B max and K d) were analyzed. In vitro stability and in vivo blood metabolism studies were also evaluated. Moreover, biodistribution studies were performed in normal and into the tumor-bearing mice at interval time points post-injection (p.i.). Both in vitro and in vivo blockade experiments were done in the presence of the σ receptors blocking agents. RESULTS:Radioiodinated ligand was obtained in high yield and high specific activity. The σ inhibition constants (K i, nM) for 4-(3-iodobenzyl)-1-(benzylsulfonyl)piperazine (4-IBBSPz), (+)-pentazocine, haloperidol, DTG, and 4-B-IBSP were 1.37 ± 0.19, 3.90 ± 0.77, 2.69 ± 0.33, 30.62 ± 2.01, and 0.61 ± 0.05, respectively. 4-B-[125I]IBSP bound to σ receptor sites preferably to very high-affinity binding sites on T47D cells. The radioligand showed acceptable in vitro and in vivo stabilities in the blood pool. However, in vivo biodistribution studies in normal Swiss albino mice revealed fast clearance of 4-B-[125I]IBSP from blood and the other normal organs. Biodistribution experiments of 4-B-[125I]IBSP in breast adenocarcinoma tumor-bearing BALB/c mice showed a relatively high tumor uptake at 30 min p.i. (4.13 ± 0.95) that reaches to 1.57 ± 0.24 even after 240 min p.i. A pre-injection of 4-B-IBSP and haloperidol with 4-B-[125I]IBSP resulted in 36-57% decrease in activity in the tumor, liver, and brain at 60 min p.i. CONCLUSIONS:The high affinity of 4-B-[125I]IBSP to σ receptor-binding sites, its relatively high uptake, and preferential retention in the tumor as well as an increasing trend observed in the tumor to blood and in the tumor to muscle ratios suggests that an iodine-123 labeled counterpart, 4-B-[123I]IBSP, would be a promising σ radioligand for pursuing further studies to assess its potential for breast tumors imaging with SPECT.
journal_name
Ann Nucl Medjournal_title
Annals of nuclear medicineauthors
Sadeghzadeh M,Alirezapour B,Charkhlooie GA,Baghery MK,Khorouti Adoi
10.1007/s12149-017-1161-8subject
Has Abstractpub_date
2017-05-01 00:00:00pages
335-346issue
4eissn
0914-7187issn
1864-6433pii
10.1007/s12149-017-1161-8journal_volume
31pub_type
杂志文章abstract:OBJECTIVE:Vesicoureteral reflux (VUR) is a major risk factor for recurrent symptomatic urinary tract infection (UTI) in pediatric patients. In addition, dimercaptosuccinic acid renal scintigraphy (DMSA) is an important diagnostic modality of VUR. However, the value of DMSA for predicting recurrent pediatric UTI has not...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-019-01379-0
更新日期:2019-09-01 00:00:00
abstract:BACKGROUND:Rest thallium-201 (201Tl) myocardial perfusion imaging has been widely used for evaluation of myocardial ischemia/viability after myocardial infarction, but the ideal timing for imaging after injection to maximally estimate viability is not well established. METHODS:Thirty-six patients with myocardial infar...
journal_title:Annals of nuclear medicine
pub_type: 临床试验,杂志文章
doi:10.1007/BF02985586
更新日期:2006-01-01 00:00:00
abstract::Tuberculosis peritonitis is a rare manifestation of extrapulmonary tuberculosis. The results of gallium-67 scintigraphy of three patients with tuberculosis peritonitis were reviewed to assess its usefulness in the diagnosis of this condition. Tuberculosis peritonitis was associated with diffuse or focal abdominal loca...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/BF03164860
更新日期:1999-06-01 00:00:00
abstract:OBJECTIVE:On hepatobiliary scintigraphy, "preferential gallbladder (GB) filling without tracer excretion into the small bowel (SB) [p-GB-no-SB]" is occasionally seen on images obtained up to an hour. In such cases, many practitioners administer cholecystokinin (CCK) (even when the measurement of GB ejection fraction is...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-019-01384-3
更新日期:2019-10-01 00:00:00
abstract:OBJECTIVES:This study investigated the prognostic value of preoperative breast-specific gamma imaging (BSGI) uptake measured by a semi-quantitative method in invasive ductal carcinoma (IDC). METHODS:One hundred and sixty-two women with IDC who underwent preoperative BSGI were retrospectively enrolled. The tumor-to-nor...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-015-0977-3
更新日期:2015-08-01 00:00:00
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
doi:10.1007/BF02996296
更新日期:2002-05-01 00:00:00
abstract:OBJECTIVE:The aim of this study was to measure the apparent diffusion coefficient (ADC) value at the region with the highest FDG uptake using sequential (18)F-FDG PET and MRI, and to correlate it with the histological grade of invasive ductal carcinoma (IDC) of the breast. METHODS:A retrospective study was conducted o...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-013-0737-1
更新日期:2013-10-01 00:00:00
abstract::Fine 2-deoxy-2-[18F]fluoro-D-glucose (18FDG) powder was obtained by adding diethyl ether into a methyl alcohol solution of 18FDG and other sugar as seed. When micronized particles of sodium N-acetyl-neuraminate (Neu5Ac-Na) were used as seed crystals, particles containing 18FDG were obtained and 80% of them were smalle...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/BF03178301
更新日期:1989-11-01 00:00:00
abstract:OBJECTIVE:In mCRPC patients treated with 223Ra, a major issue is the validation of reliable prognostic and predictive biomarkers to maximize clinical benefit and minimize toxicities and costs. Bearing in mind how changes in tALP did not meet statistical requirements as surrogate marker for survival, aim of this single-...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-017-1228-6
更新日期:2018-02-01 00:00:00
abstract:OBJECTIVE:To clarify the difference of (18)F-FDG uptake kinetics between FDG-avid metastatic lymph nodes (LNs) in patients with non-small-cell lung cancer (NSCLC) and FDG-avid benign LNs associated with various etiologies on dual-time point PET/CT scan, and to determine the optimal parameter for differentiation. METHO...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-009-0268-y
更新日期:2009-08-01 00:00:00
abstract::99mTc-tetrofosmin, Thallium-201-chloride (201Tl) and 99mTc-MIBI imagings were performed in a patient with malignant thymoma. Tracer uptake in the primary tumor was demonstrated. The tumor-to-background ratios of planar and SPECT imagings were 1.60 and 1.98 for 99mTc-tetrofosmin, 1.12 and 2.09 for 201Tl, and 1.19 and 1...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/BF02988212
更新日期:2000-08-01 00:00:00
abstract:OBJECTIVES:Cardiac resynchronization therapy (CRT) is the established treatment for patients with chronic and severe heart failure, and it has been reported that the presence of left ventricular (LV) dyssynchrony is one of the most important factors which predict positive response of this therapy. In the present study,...
journal_title:Annals of nuclear medicine
pub_type: 临床试验,杂志文章
doi:10.1007/s12149-011-0525-8
更新日期:2011-12-01 00:00:00
abstract::Most of the acute ischemic events, such as acute coronary syndromes and stroke, are attributed to vulnerable plaques. These lesions have common histological and pathophysiological features, including inflammatory cell infiltration, neo-angiogenesis, remodelling, haemorrhage predisposition, thin fibrous cap, large lipi...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章,评审
doi:10.1007/s12149-020-01458-7
更新日期:2020-05-01 00:00:00
abstract:OBJECTIVE:To investigate the potential role of Tc-99m depreotide (Tc-DEPR) in the preoperative lymph node (N) staging of non-small-cell lung cancer (NSCLC). METHODS:Sixty-one patients with NSCLC at the potentially operable stage were enrolled and underwent scintigraphy before surgery (n=56) or mediastinoscopy (n=5). I...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-014-0839-4
更新日期:2014-06-01 00:00:00
abstract:OBJECTIVE:Iodine-123-labeled N-isopropyl-4-iodoamphetamine (IMP) is used as a tracer for the measurement of cerebral blood flow (CBF) by single-photon emission computed tomography (SPECT). Two IMP products, IMP(A) (Nihon Medi-Physics Co., Ltd.) and IMP(B) (FUJIFILM RI Pharma Co., Ltd.), produced by different radiopharm...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-009-0242-8
更新日期:2009-06-01 00:00:00
abstract:OBJECTIVE:To compare histological findings of FDG-PET false-positive and true-negative hilar and mediastinal lymph nodes. METHODS:Sixty-seven lymphnode areas in 11 patients who were diagnosed to have N3 lymph nodes by FDG-PET and underwent surgery were histologically examined, and the histopathological findings in fal...
journal_title:Annals of nuclear medicine
pub_type: 临床试验,杂志文章
doi:10.1007/BF02985610
更新日期:2004-02-01 00:00:00
abstract:OBJECTIVE:One mechanism that may be responsible for drug resistance in epilepsy is the upregulation of P-glycoprotein (P-gp), a drug efflux pump, at the epileptogenic focus. In this study, we sought to evaluate the potential of a recently developed P-gp PET radiotracer, [(11)C]N-desmethyl-loperamide ([(11)C]dLop), for ...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-013-0725-5
更新日期:2013-08-01 00:00:00
abstract::We report a functional neuroimaging study of a patient clinically diagnosed with Korsakoff syndrome. Positron emission tomography (PET) with the 15O inhalation method showed decreased regional cerebral blood flow (rCBF) and decreased regional cerebral metabolic ratio for oxygen (rCMRO2) in the bilateral fronto-tempora...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/BF03164755
更新日期:1997-02-01 00:00:00
abstract:PURPOSE:Treatment effect of radiofrequency ablation (RFA) is traditionally accomplished with MRI and/or CT. The aim of the study was to assess the role of FDG-PET in post RFA hepatic tumor evaluation, in comparison with MRI and CT. MATERIALS AND METHODS:28 patients (33 hepatic RFA lesions) who had post RFA FDG-PET wit...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-012-0656-6
更新日期:2013-01-01 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::Myocardial normal databases for stress myocardial perfusion study have been created by the Japanese Society of Nuclear Medicine Working Group. The databases comprised gender-, camera rotation range- and radiopharmaceutical-specific data-sets from multiple institutions, and normal database files were created for instal...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章,评审
doi:10.1007/s12149-009-0337-2
更新日期:2010-04-01 00:00:00
abstract:OBJECTIVE:To evaluate the value of Bayesian penalized likelihood (BPL) reconstruction for improving lesion conspicuity of malignant lung tumors on 18F-fluoro-2-deoxy-D-glucose (FDG) positron emission tomography computed tomography (PET/CT) as compared with the ordered subset expectation maximization (OSEM) reconstructi...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-020-01446-x
更新日期:2020-04-01 00:00:00
abstract::A case of Plummer's disease that spontaneously progressed to hypothyroidism is presented. A 49-year-old female visited our hospital because of a 3 kg decrease in body weight during the previous month and a painless nodule in the right anterior area of her neck. A diagnosis of Plummer's disease was made based on the re...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/BF03164940
更新日期:1999-12-01 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: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: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:OBJECTIVE:A complication after spinal fusion surgery is pseudarthrosis, but its radiological diagnosis is of limited value. (18)F-fluoride PET with its ability to assess bone metabolism activity could be of value. The goal of this study was to assess the clinical feasibility of calculating the static standardized uptak...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-015-1008-0
更新日期:2015-11-01 00:00:00
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
doi:10.1007/BF03164899
更新日期:1999-08-01 00:00:00
abstract::HIV infection results in profound alterations of immunologic function that render the patient severely immunocompromised, and susceptible to malignancies and opportunistic infections. Three AIDS-defining malignancies include Kaposi's sarcoma (KS), non-Hodgkin's lymphoma (NHL) and invasive cervical cancer. In AIDS pati...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章,评审
doi:10.1007/s12149-011-0506-y
更新日期:2011-10-01 00:00:00
abstract:PURPOSE:The aim of this study was to elucidate the regional differences between brain perfusion single photon emission computed tomography (SPECT) images reconstructed with a uniform attenuation correction using Chang's method (AC-Chang) and a non-uniform attenuation correction with CT using SPECT/CT (AC-CT). METHODS:...
journal_title:Annals of nuclear medicine
pub_type: 杂志文章
doi:10.1007/s12149-011-0567-y
更新日期:2012-04-01 00:00:00