Abstract:
PURPOSE:[(18)F]Flumazenil, which has the advantage of a longer half-life than [(11)C]flumazenil, is well known for determining of the central benzodiazepine receptor concentrations. However, [(18)F]flumazenil has not been widely used because fluctuating and relatively low yields render automatic production insufficient for routine and multicenter clinical trials. Here, we describe the results of a 2.5-year production study of [(18)F]flumazenil using an iodonium tosylate precursor, which allowed us to overcome the limitations of low and fluctuating radiochemical yields. PROCEDURES:We developed a clinically applicable production system by modifying a commercial synthesizer for the reliable and reproducible production of [(18)F]flumazenil for routine clinical studies. [(18)F]Flumazenil was prepared at 150 °C for 5 min in the presence of 4-methylphenyl-mazenil iodonium tosylate (4 mg), a radical scavenger (TEMPO, 1 mg), and [(18)F]KF/kryptofix 2.2.2 complex in N,N-dimethylformamide (1 ml). In the purification step, the final mixture was pretreated using different cartridges before performing high-performance liquid chromatography (HPLC) separation. Finally, we measured the radiochemical yield and performed quality-control assays on 94 batches. RESULTS:After carrying out additional purification before HPLC separation using a C18 plus Sep-Pak cartridge, the radiochemical yield of [(18)F]flumazenil increased from 34.4 ± 9.7 % (without the pretreatment, n = 24) to 53.4 ± 9.0 % (n = 94), and the lifetime of the semi-preparative column was five times that of the column without the C18 plus Sep-Pak cartridge. The mean-specific activity of [(18)F]flumazenil was 572 ± 116 GBq/μmol at the end of synthesis, and the radiochemical purity was more than 99 %, as determined by analytical HPLC and radio-TLC. [(18)F]Flumazenil prepared using this method satisfied all quality-control test standards and was highly stable for up to 6 h after preparation. CONCLUSIONS:The results of the 2.5-year production study using an iodonium tosylate precursor indicate that [(18)F]flumazenil has commercial and routine clinical applicability.
journal_name
Mol Imaging Bioljournal_title
Molecular imaging and biologyauthors
Moon BS,Park JH,Lee HJ,Lee BC,Kim SEdoi
10.1007/s11307-014-0738-zsubject
Has Abstractpub_date
2014-10-01 00:00:00pages
619-25issue
5eissn
1536-1632issn
1860-2002journal_volume
16pub_type
杂志文章abstract:PURPOSE:Many radioligands have been explored for imaging the 18-kDa translocator protein (TSPO), a diagnostic and therapeutic target for inflammation and cancer. Here, we investigated the TSPO radioligand [(18)F]DPA-714 for positron emission tomography (PET) imaging of cancer and inflammation. PROCEDURES:[(18)F]DPA-71...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-015-0877-x
更新日期:2016-02-01 00:00:00
abstract:PURPOSE:The purpose of this study was to investigate the feasibility of dual magnetic resonance imaging (MRI) reporter genes, including ferritin heavy subunit (Fth) and transferrin receptor (TfR), which provide sufficient MRI contrast for in vivo MRI tracking, and the Deltex-1 (DTX1) gene, which promotes human mesenchy...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-017-1128-0
更新日期:2018-06-01 00:00:00
abstract:PURPOSE:The increasing availability of fluorescent probes for in vivo optical imaging enables the interrogation of complex biological processes in small animals serving as models for human-like tissue function and disease. However, the validation of probe bio-distribution during their development or the study of differ...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-010-0416-8
更新日期:2011-10-01 00:00:00
abstract:PURPOSE:Widely used in clinical practice, the maximum standardized uptake value (SUVmax) is a statistical index highly prone to physical and biological variations, which can lead to unpredictable errors. This study has a methodological aim: to identify a more robust SUV-based index representing the tracer accumulation....
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-019-01451-1
更新日期:2020-08-01 00:00:00
abstract:PURPOSE:The aim of this study is to evaluate the impact of different scatter correction strategies on quantification of high-resolution research tomograph (HRRT) data for three tracers covering a wide range in kinetic profiles. PROCEDURES:Healthy subjects received dynamic HRRT scans using either (R)-[(11)C]verapamil (...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-015-0921-x
更新日期:2016-08-01 00:00:00
abstract:PURPOSE:Prostate-specific membrane antigen (PSMA) continues to be the hallmark biomarker for prostate cancer as it is expressed on nearly all prostatic tumors. In addition, increased PSMA expression correlates with castration resistance and progression to the metastatic stage of the disease. Recently, we combined both ...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-019-01404-8
更新日期:2020-04-01 00:00:00
abstract:PURPOSE:Visualization of tumor necrosis can determine tumor response to therapy. Our previous study showed that the rhein-based magnetic resonance imaging (MRI) contrast agent with alkane linker (GdL2) could clearly image tumor necrosis. However, its water solubility and cell safety needed to be improved. Herein, three...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-020-01551-3
更新日期:2020-10-13 00:00:00
abstract:PURPOSE:To investigate the prognostic performance of radiomics features, as extracted from positron emission tomography (PET) and X-ray computed tomography (CT) components of baseline 2-deoxy-2-[18F]fluoro-D-glucose ([18F]FDG) PET/CT images and integrated with clinical parameters, in patients with nasopharyngeal carcin...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-018-01304-3
更新日期:2019-10-01 00:00:00
abstract:PURPOSE:Previous reports confirmed that (2S,4R)-4-[18F]Fluoroglutamine ([18F]GLN) accumulated in bone and bone marrow. This study investigates the potential of using [18F]GLN positron emission tomography (PET) to monitor changes of bone marrow activity after chemotherapy (myelosuppression). PROCEDURES:Bone marrow inhi...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-019-01319-4
更新日期:2019-10-01 00:00:00
abstract::Positron emission tomography (PET) with epidermal growth factor receptor (EGFR) kinase-specific radiolabeled tracers could provide the means for noninvasive and repetitive imaging of heterogeneity of EGFR expression and signaling activity in tumors in individual patients before and during therapy with EGFR signaling i...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-006-0049-0
更新日期:2006-09-01 00:00:00
abstract:PURPOSE:Previous studies has demonstrated the utility of human epidermal growth factor receptor type 2 (HER2) as an attractive target for cancer molecular imaging and therapy. An affibody protein with strong binding affinity for HER2, ZHER2:342, has been reported. Various methods of chelator conjugation for radiolabeli...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-018-01310-5
更新日期:2019-10-01 00:00:00
abstract:PURPOSE:Angiogenesis is essential for physiological processes as well as for carcinogenesis. New approaches to cancer therapy include targeting angiogenesis. One target is VEGF-A and its receptor VEGFR2. In this study, we sought to investigate pancreatic cancer angiogenesis in a genetically modified VEGFR2-luc-KI mouse...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-010-0310-4
更新日期:2010-12-01 00:00:00
abstract:PURPOSE:The tyrosine kinase receptor Axl is overexpressed in various types of cancer and correlated with cancer malignancy. Selective Axl blockade reduces tumor growth and metastasis. The purpose of this study was to examine whether the humanized anti-Axl antibody humanized 173 (h173) labeled with near-infrared fluores...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-013-0714-z
更新日期:2014-08-01 00:00:00
abstract:PURPOSE:Sensitivity of contrast-enhanced ultrasound (CEUS) to microvascular flow modifications can be limited by intra-injection variability (injected dose, rate, volume). PROCEDURES:To evaluate the effect of injection variability on microvascular flow evaluation, CEUS was compared between controlled and manual inject...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-016-0952-y
更新日期:2016-10-01 00:00:00
abstract:PURPOSE:We examine the feasibility of fluorescent imaging system for sentinel lymph node detection by using functionalized silica nanoparticles. MATERIALS AND METHODS:We developed a functionalized RITC-SiO(2) nanoparticles containing fluorescent dye, C(28)H(31)N(2)O(3)Cl (rhodamine B isothiocyanate) inside, and subseq...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-009-0262-8
更新日期:2010-04-01 00:00:00
abstract:PURPOSE:Diabetes is associated with a deterioration of the microvasculature in brown adipose tissue (BAT) and with a decrease in its metabolic activity. Multispectral optoacoustic tomography has been recently proposed as a new tool capable of differentiating healthy and diabetic BAT by observing hemoglobin gradients an...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-018-1291-y
更新日期:2019-08-01 00:00:00
abstract:PURPOSE:This study describes an imaging strategy based on glow stick chemistry to non-invasively image oxidative stress and reactive oxygen species (ROS) production in living animals. PROCEDURES:Upon stimulation, phagocytes produce toxic levels of ROS to kill engulfed microorganisms. The mitochondrial respiratory chai...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-014-0721-8
更新日期:2014-08-01 00:00:00
abstract:PURPOSE:Repetitive imaging with microPET of endogenous albumin gene expression by using transgenic mice in which the Herpes Simplex Virus Type 1 thymidine kinase (HSV1-tk) reporter gene is driven by the albumin promoter (AL-HSV1-tk). METHODS:Transgenic mice were imaged repeatedly on a microPET scanner with approximate...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1016/s1095-0397(01)00071-1
更新日期:2002-01-01 00:00:00
abstract::Morphological imaging techniques are typically used in the anti-cancer drug efficacy evaluation process. However, these techniques can evaluate the therapeutic efficacy only when the tumor shows anatomic changes-usually at later stages, when the therapeutic effects are poor. In contrast, molecular imaging allows nonin...
journal_title:Molecular imaging and biology
pub_type: 杂志文章,评审
doi:10.1007/s11307-019-01431-5
更新日期:2020-12-01 00:00:00
abstract:PURPOSE:Evaluation of [68Ga]NODAGA-duramycin as a positron emission tomography (PET) tracer of cell death for whole-body detection of chemotherapy-induced organ toxicity. PROCEDURES:Tracer specificity of Ga-68 labeled NODAGA-duramycin was determined in vitro using competitive binding experiments. Organ uptake was anal...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-019-01417-3
更新日期:2020-06-01 00:00:00
abstract:PURPOSE:Human pluripotency gene networks (PGNs), controlled in part by Oct4, are central to understanding pluripotent stem cells, but current fluorescent reporter genes (RGs) preclude noninvasive assessment of Oct4 dynamics in living subjects. PROCEDURES:To assess Oc4 activity noninvasively, we engineered a mouse embr...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-014-0744-1
更新日期:2014-12-01 00:00:00
abstract:PURPOSE:Vulnerable plaques are key factors for ischemic diseases. Thus, their precise detection is necessary for the diagnosis of such diseases. Immunoglobulin G (IgG)-based imaging probes have been developed for imaging biomolecules related to plaque formation for the diagnosis of atherosclerosis. However, IgG accumul...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-016-1036-8
更新日期:2017-08-01 00:00:00
abstract:PURPOSE:Antibodies form an important class of cancer therapeutics, and there is intense interest in using them for imaging applications in diagnosis and monitoring of cancer treatment. Despite the expanding body of knowledge describing pharmacokinetic and pharmacodynamic interactions of antibodies in vivo, discrepancie...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-010-0397-7
更新日期:2011-08-01 00:00:00
abstract:PURPOSE:Inflammation plays a key role in the progression of intervertebral disk (IVD) herniation and associated low back pain. However, real-time spatial diagnosis of inflammation associated with acute disk herniation has not been investigated. We sought to detect local neutrophil and macrophage infiltration near disk ...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-016-1038-6
更新日期:2017-10-01 00:00:00
abstract:PURPOSE:The aim of this work is to investigate the impact of tissue classification in magnetic resonance imaging (MRI)-guided positron emission tomography (PET) attenuation correction (AC) for whole-body (WB) Patlak net uptake rate constant (Ki) imaging in PET/MRI studies. PROCEDURES:WB dynamic PET/CT data were acquir...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-019-01338-1
更新日期:2019-12-01 00:00:00
abstract::The article "Pre-therapy Somatostatin Receptor-Based Heterogeneity Predicts Overall Survival in Pancreatic Neuroendocrine Tumor Patients Undergoing Peptide Receptor Radionuclide Therapy," was originally published electronically on the publisher's internet portal without open access. ...
journal_title:Molecular imaging and biology
pub_type: 杂志文章,已发布勘误
doi:10.1007/s11307-018-1261-4
更新日期:2018-12-01 00:00:00
abstract:PURPOSE:We recently reported that high thymidine phosphorylase (TP) expression is accompanied by low tumor thymidine concentration and high 3'-deoxy-3'-[18F]fluorothymidine ([18F]FLT) uptake in four untreated lung cancer xenografts. Here, we investigated whether this relationship also holds true for a broader range of ...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-017-1125-3
更新日期:2018-04-01 00:00:00
abstract:PURPOSE:Positron emission tomography (PET) with 2-deoxy-2-[18F]fluoro-D-glucose (FDG) has been used for various cancers, but reproducibility of common utilized semi-quantitative parameters, such as the maximal single pixel standardized uptake value (SUV) and effective glycolytic volume (EGV), remains unknown. Knowledge...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1016/s1536-1632(01)00004-x
更新日期:2002-03-01 00:00:00
abstract:PURPOSE:Carbon ion radiotherapy (CIRT) has been developed, and a phase I/II CIRT trial has been conducted in patients with adenocarcinoma in the head and neck region. We evaluated whether the L-methyl [11C]-methionine (MET) uptake could be an early predictor for local recurrence, metastasis, and the prognosis in patien...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-010-0318-9
更新日期:2010-10-01 00:00:00
abstract:PURPOSE:To evaluate the utility of three-dimensional (3D) amide proton transfer-weighted (APTw) imaging for differentiation of endometrial adenocarcinoma and uterine benign lesions. PROCEDURES:This prospective study enrolled 22 normal volunteers and 113 patients with suspicious uterine lesions, including endometrial a...
journal_title:Molecular imaging and biology
pub_type: 杂志文章
doi:10.1007/s11307-020-01565-x
更新日期:2020-11-13 00:00:00