Abstract:
PURPOSE:The serotonin-1A (5-HT(1A)) receptor is implicated in the pathophysiology of major neuropsychiatric disorders. Thus, the functional imaging of 5-HT(1A) receptors by positron emission tomography (PET) may contribute to the understanding of its role in those pathologies and their therapeutics. These receptors exist in high- and low-affinity states and it is proposed that agonists bind preferentially to the high-affinity state of the receptor and therefore could provide a measure of the functional 5-HT(1A) receptors. Since all clinical PET 5-HT(1A) radiopharmaceuticals are antagonists, it is of great interest to develop a( 18)F labelled agonist. METHODS:F15599 (3-chloro-4-fluorophenyl-(4-fluoro-4{[(5-methyl-pyrimidin-2-ylmethyl)-amino]-methyl}-piperidin-1-yl)-methanone) is a novel ligand with high affinity and selectivity for 5-HT(1A) receptors and is currently tested as an antidepressant. In pharmacological tests in rat, it exhibits preferential agonist activity at post-synaptic 5-HT(1A) receptors in cortical brain regions. Here, its nitro-precursor was synthesised and radiolabelled via a fluoronucleophilic substitution. Radiopharmacological evaluations included in vitro and ex vivo autoradiography in rat brain and PET scans on rats and cats. Results were compared with simultaneous studies using [(18)F]MPPF, a validated 5-HT(1A) antagonist radiopharmaceutical. RESULTS:The chemical and radiochemical purities of [(18)F]F15599 were >98%. In vitro [(18)F]F15599 binding was consistent with the known 5-HT(1A) receptors distribution (hippocampus, dorsal raphe nucleus, and notably cortical areas) and addition of Gpp(NH)p inhibited [(18)F]F15599 binding, consistent with a specific binding to G protein-coupled receptors. In vitro binding of [(18)F]F15599 was blocked by WAY100635 and 8-OH-DPAT, respectively, prototypical 5-HT(1A) antagonist and agonist. The ex vivo and in vivo studies demonstrated that the radiotracer readily entered the rat and the cat brain and generated few brain radioactive metabolites. Remarkably, in microPET studies, [(18)F]F15599 notably displayed a pattern of brain labelling that did not correlate with in vitro observations. Thus, in cat, the highest binding was observed in dorsal raphe and cingulate cortex with little binding in other cortical regions and none in hippocampus. In vivo binding was abolished by WAY100635, indicating specific labelling of 5-HT(1A) receptors. CONCLUSION:[(18)F]F15599 is a radiofluorinated agonist presenting interesting characteristics for probing in vitro and in vivo the high-affinity states of the 5-HT(1A) receptors. Its differential labelling of 5-HT(1A) receptors in vitro and in vivo may result from its reported preferential interaction with receptors coupled to specific G-protein subtypes.
journal_name
Eur J Nucl Med Mol Imagingauthors
Lemoine L,Verdurand M,Vacher B,Blanc E,Le Bars D,Newman-Tancredi A,Zimmer Ldoi
10.1007/s00259-009-1274-ysubject
Has Abstractpub_date
2010-03-01 00:00:00pages
594-605issue
3eissn
1619-7070issn
1619-7089journal_volume
37pub_type
杂志文章abstract:PURPOSE:To compare the clinical performance of upper abdominal PET/DCE-MRI with and without concurrent respiratory motion correction (MoCo). METHODS:MoCo PET/DCE-MRI of the upper abdomen was acquired in 44 consecutive oncologic patients and compared with non-MoCo PET/MRI. SUVmax and MTV of FDG-avid upper abdominal mal...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-018-4084-2
更新日期:2018-11-01 00:00:00
abstract:PURPOSE:The aim of this study was to investigate metabolic and textural parameters from pretreatment [(18)F]FDG PET/CT scans for the prediction of neoadjuvant radiation chemotherapy response and 3-year disease-free survival (DFS) in patients with locally advanced rectal cancer (LARC). METHODS:We performed a retrospect...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-015-3180-9
更新日期:2016-03-01 00:00:00
abstract:PURPOSE:PET has been proven to be helpful in the delineation of gross tumour volume (GTV) for external radiation therapy in several tumour entities. The aim of this study was to determine if [(11)C]choline PET could be used to localize the carcinomatous tissue within the prostate in order to specifically target this ar...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-013-2345-7
更新日期:2013-06-01 00:00:00
abstract:PURPOSE:Trastuzumab (Herceptin™) is often internalized following binding to Her2+ tumor cells. The objective of this study was to investigate whether trastuzumab can be used as a specific carrier to deliver antisense oligomers into Her2+ tumor cells both in vitro and in vivo. METHODS:A biotinylated MORF oligomer antis...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-009-1201-2
更新日期:2009-12-01 00:00:00
abstract:PURPOSE:Paired imaging/therapy with radiolabeled somatostatin receptor (SSTR) antagonists is a novel approach in neuroendocrine tumors (NETs). The aim of this study was to compare tumor uptake of 68Ga-DOTA-JR11 and 177Lu-satoreotide tetraxetan (177Lu-DOTA-JR11) in patients with NETs. METHODS:As part of a prospective c...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-020-04832-9
更新日期:2020-12-01 00:00:00
abstract:PURPOSE:Radionuclide renography with angiotensin converting enzyme (ACE) inhibition plays an important role in the diagnosis of haemodynamically significant renal artery stenosis. Angiotensin receptor antagonists inhibit the renin angiotensin system at different levels from ACE inhibitors by selectively blocking the bi...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 临床试验,杂志文章
doi:10.1007/s00259-005-1789-9
更新日期:2005-09-01 00:00:00
abstract:PURPOSE:Prostate-specific membrane antigen (PSMA) positron emission tomography (PET)/computed tomography (CT) is used for (re)staging prostate cancer (PCa) and as a biomarker for evaluating response to therapy, but lacks established response criteria. A panel of PCa experts in nuclear medicine, radiology, and/or urolog...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-020-04934-4
更新日期:2021-02-01 00:00:00
abstract:PURPOSE:To study the effect of adjuvant lithium on serum thyroxine (T4) concentrations in patients treated with radioactive iodine (RAI) therapy in our environment. METHODS:This was a prospective simple randomized comparative, experimental cohort study of patients with hyperthyroidism referred for RAI ablation therapy...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章,多中心研究,随机对照试验
doi:10.1007/s00259-016-3388-3
更新日期:2016-10-01 00:00:00
abstract::Flow quantitation with nitrogen-13 ammonia ((13)NH(3)) and positron emission tomography (PET) is dependent on an accurate blood time-activity curve. This is conveniently derived from the PET images by drawing a region of interest in the left ventricular cavity. The blood time-activity curve obtained in this way, howev...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 临床试验,杂志文章
doi:10.1007/s00259-003-1329-4
更新日期:2004-01-01 00:00:00
abstract:PURPOSE:Chemoradiotherapy is the reference curative-intent treatment for nonresectable locally advanced non-small-cell lung carcinoma (NSCLC), with unsatisfactory survival, partially due to radiation resistance in hypoxic tissues. The objective was to update survival and toxicity at 3 years following radiotherapy boost...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章,多中心研究
doi:10.1007/s00259-019-04285-9
更新日期:2019-07-01 00:00:00
abstract:PURPOSE:The purpose of this study was to evaluate therapeutic response to neoadjuvant chemotherapy (NAC) and predict breast cancer recurrence using Positron Emission Tomography Response Criteria in Solid Tumors (PERCIST). MATERIALS AND METHODS:Fifty-nine breast cancer patients underwent fluorodeoxyglucose-positron emi...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章,多中心研究
doi:10.1007/s00259-018-4008-1
更新日期:2018-09-01 00:00:00
abstract:PURPOSE:(11)C-methionine (MET) PET is an established diagnostic tool for glioma. Studies have suggested that MET uptake intensity in the tumor is a useful index for predicting patient outcome. Because MET uptake is known to reflect tumor expansion more accurately than MRI, we aimed to elucidate the association between ...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-015-3046-1
更新日期:2015-06-01 00:00:00
abstract:PURPOSE:Functional activation protocols are widely applied for the study of brain-cognition relations. Only few take advantage of the intrinsic characteristics of SPECT, particularly those allowing cognitive assessment outside of the camera, in settings close to the standard clinical or laboratory ones. The purpose of ...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-007-0635-7
更新日期:2008-04-01 00:00:00
abstract::We here aim to provide a comprehensive and critical review of the literature concerning the clinical applications of positron emission tomography/computed tomography (PET/CT) with radiolabeled choline in patients with prostate cancer (PCa). We will initially briefly summarize the historical context that brought to the...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章,评审
doi:10.1007/s00259-017-3700-x
更新日期:2017-09-01 00:00:00
abstract:PURPOSE:To investigate the value of 68Ga-HBED-CC PSMA (68Ga-PSMA) PET/CT for response assessment in metastatic castration-sensitive and castration-resistant prostate cancer (mCSPC and mCRPC) during docetaxel chemotherapy. METHODS:68Ga-PSMA PET/CT was performed in seven mCSPC patients before and after six cycles of upf...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-017-3887-x
更新日期:2018-04-01 00:00:00
abstract::This study demonstrates high-efficiency sterilisation of single cancer cells in a SCID mouse model of leukaemia using rituximab, a monoclonal antibody that targets CD20, labelled with terbium-149, an alpha-emitting radionuclide. Radio-immunotherapy with 5.5 MBq labelled antibody conjugate (1.11 GBq/mg) 2 days after an...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-003-1413-9
更新日期:2004-04-01 00:00:00
abstract:PURPOSE:This study aimed at identifying prior therapy dosimetric parameters using 99mTc-labeled macro-aggregates of albumin (MAA) that are associated with contralateral hepatic hypertrophy occurring after unilobar radioembolization of hepatocellular carcinoma (HCC) performed with 90Y-loaded glass microspheres. METHODS...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-017-3845-7
更新日期:2018-03-01 00:00:00
abstract:BACKGROUND:The aim of this study was to assess radiomics features on pre-treatment [18F]FDG positron emission tomography (PET) as potential biomarkers for response and survival in patients with metastatic colorectal cancer (mCRC). METHODS:Patients with mCRC underwent [18F]FDG PET/computed tomography (CT) prior to firs...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-018-4100-6
更新日期:2018-12-01 00:00:00
abstract:PURPOSE:To determine the value of (68)Ga-DOTA-TOC and (18)F-FDG PET/CT for initial and follow-up evaluation of patients with neuroendocrine tumour (NET) treated with peptide receptor radionuclide therapy (PRRT). METHODS:We evaluated 66 patients who had histologically proven NET and underwent both PRRT and three combin...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-016-3328-2
更新日期:2016-08-01 00:00:00
abstract:PURPOSE:To assess the relationship between serum thyroglobulin (Tg) levels, Tg doubling time (Tg-DT) and the diagnostic performance of (18)F-FDG PET/CT in detecting recurrences of (131)I-negative differentiated thyroid carcinoma (DTC). METHODS:Included in the present study were 102 patients with DTC. All patients were...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-013-2370-6
更新日期:2013-06-01 00:00:00
abstract:INTRODUCTION:Mastocytosis is a clonal haematological disease characterized by uncontrolled proliferation and the activation of mast cells. The value of FDG-PET/CT (FDG-PET) in mastocytosis has yet to be determined. METHODS:We retrospectively identified patients with an established diagnosis of systemic mastocytosis (S...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章,多中心研究
doi:10.1007/s00259-015-3117-3
更新日期:2015-12-01 00:00:00
abstract:PURPOSE:Twelve years ago a meta-analysis evaluated the diagnostic performance of (18)F-fluorodeoxyglucose (FDG) positron emission tomography (PET) in assessing musculoskeletal soft tissue lesions (MsSTL). Currently, PET/CT has substituted PET imaging; however, there has not been any published meta-analysis on the use o...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章,meta分析,评审
doi:10.1007/s00259-015-3242-z
更新日期:2016-05-01 00:00:00
abstract::Medical imaging has made a major contribution to cerebral dysfunction due to inherited diseases, as well as injuries sustained with modern living, such as car accidents, falling down, and work-related injuries. These injuries, up until the introduction of sensitive techniques such as positron emission tomography (PET)...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章,收录出版
doi:10.1007/s00259-013-2401-3
更新日期:2013-09-01 00:00:00
abstract:PURPOSE:To review literature until November 2015 and reach a consensus on whether automatic semi-quantification of brain FDG-PET is useful in the clinical setting for neurodegenerative disorders. METHODS:A literature search was conducted in Medline, Embase, and Google Scholar. Papers were selected with a lower limit o...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章,评审
doi:10.1007/s00259-018-4030-3
更新日期:2018-07-01 00:00:00
abstract:PURPOSE:In the era of precision medicine, patient-specific dose calculation using Monte Carlo (MC) simulations is deemed the gold standard technique for risk-benefit analysis of radiation hazards and correlation with patient outcome. Hence, we propose a novel method to perform whole-body personalized organ-level dosime...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-020-05013-4
更新日期:2020-09-01 00:00:00
abstract:BACKGROUND:(131)Iodine (I131)-metaiodobenzylguanidine (mIBG) is a radionuclide-based treatment option for metastatic gastrointestinal-pancreatic neuroendocrine tumours (GEP NET). This study aimed at identifying prognostic indicators of long-term outcome based on initial evaluation following a first mIBG treatment (7400...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-015-3116-4
更新日期:2015-12-01 00:00:00
abstract:PURPOSE:In this study, kinetic parameters of the cellular proliferation tracer (18)F-3'-deoxy-3'-fluoro-L-thymidine (FLT) and the amino acid probe 3,4-dihydroxy-6-(18)F-fluoro-L-phenylalanine (FDOPA) were measured before and early after the start of therapy, and were used to predict the overall survival (OS) of patient...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-013-2678-2
更新日期:2014-06-01 00:00:00
abstract:PURPOSE:In children with Hodgkin's disease and non-Hodgkin's lymphoma, the ability of (18)F-fluoro-2-deoxy-D-glucose PET/CT and conventional imaging (CI) to detect malignant lesions and predict poor lesion response to therapy was assessed and compared. METHODS:A retrospective review of findings reported on PET/CT and ...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-010-1619-6
更新日期:2011-02-01 00:00:00
abstract:PURPOSE:Our study intended to explore the association between combining 18F-FDG PET/CT metabolic parameters and other clinical features and anaplastic lymphoma kinase (ALK) or c-ros oncogene 1 (ROS1) fusion in non-small-cell lung cancer (NSCLC). METHODS:Eight hundred and six patients with wild-type epidermal growth fa...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-019-04652-6
更新日期:2020-05-01 00:00:00
abstract::The iodinated cocaine derivative [(123)I]PE2I is a new selective ligand for in vivo studies of the dopamine transporter (DAT) with single-photon emission tomography (SPET). The aim of the present study was to describe a method for accurate quantification of binding data following a bolus injection of [(123)I]PE2I. Six...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 临床试验,杂志文章
doi:10.1007/s00259-001-0742-9
更新日期:2002-05-01 00:00:00