Abstract:
PURPOSE:Brain serotonin 6 receptor (5-HT6) is one of the most recently identified serotonin receptors. It is a potent therapeutic target for psychiatric and neurological diseases, e.g. schizophrenia and Alzheimer's disease. Since no specific fluorinated radioligand has yet been successfully used to study this receptor by positron emission tomography (PET) neuroimaging, the objective of the present study was to study the first 5-HT6 (18)F-labelled radiotracer. METHODS:2FNQ1P, inspired by the quinolone core of a previous radiotracer candidate, GSK215083, was selected according its 5-HT6 affinity and selectivity and was radiolabelled by (18)F nucleophilic substitution. The cerebral distribution of [(18)F]2FNQ1P was studied in vivo in rats, cats and macaque monkeys. RESULTS:The chemical and radiochemical purities of [(18)F]2FNQ1P were >98 %. In rats, in vitro competition with the 5-HT6 antagonist, SB258585, revealed that the radioligand was displaced dose dependently. Rat microPET studies showed low brain uptake of [(18)F]2FNQ1P, reversed by the P-glycoprotein inhibitor, cyclosporin. On the contrary, PET scans in cats showed good brain penetration and specific striatal binding blocked after pretreatment with unlabelled 2FNQ1P. PET scans in macaque monkeys confirmed high specific binding in both cortical and subcortical regions, specifically decreased by pretreatment with the 5-HT6 receptor antagonist, SB258585. CONCLUSION:2FNQ1P was initially selected because of its suitable characteristics for 5-HT6 receptor probing in vitro in terms of affinity and specificity. Although in vivo imaging in rats cannot be considered as predictive of the clinical characteristics of the radiotracer, [(18)F]2FNQ1P appeared to be a suitable 5-HT6 PET tracer in feline and primate models. These preclinical results encourage us to pursue the clinical development of this first fluorinated 5-HT6 PET radiotracer.
journal_name
Eur J Nucl Med Mol Imagingauthors
Becker G,Colomb J,Sgambato-Faure V,Tremblay L,Billard T,Zimmer Ldoi
10.1007/s00259-014-2936-ysubject
Has Abstractpub_date
2015-03-01 00:00:00pages
495-502issue
3eissn
1619-7070issn
1619-7089journal_volume
42pub_type
杂志文章abstract:PURPOSE:According to the updated WHO classification of gliomas with its emphasis on molecular parameters, tumours with an IDH-wildtype status have a dismal prognosis. To ensure timely adjustment of treatment, demand for non-invasive prediction methods is high. 18F-FET PET has been shown to be an important diagnostic to...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-019-04477-3
更新日期:2019-11-01 00:00:00
abstract:PURPOSE:The study serves to optimise conditions for multi-pinhole SPECT small animal imaging of (123)I- and (99m)Tc-labelled radiopharmaceuticals with different distributions in murine heart and brain and to investigate detection and dose range thresholds for verification of differences in tracer uptake. METHODS:A Tri...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-009-1142-9
更新日期:2009-09-01 00:00:00
abstract:PURPOSE:The goal of this study is to determine the technical accuracy of segmental perfusion parameters assessed with quantitative cardiac PET imaging in the evaluation of coronary artery disease (CAD) in patients with stable angina. METHODS:A cohort of patients who participated in the EVINCI protocol underwent an eva...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-016-3362-0
更新日期:2016-07-01 00:00:00
abstract::Physiologically increased pancreatic uptake at the head/uncinate process is observed in more than one-third of patients after injection of one of the three (68)Ga-labelled octreotide-based peptides used for somatostatin (sst) receptor (r) imaging. There are minor differences between these (68)Ga-sstr-binding peptides ...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章,评审
doi:10.1007/s00259-016-3395-4
更新日期:2016-10-01 00:00:00
abstract:PURPOSE:The aims of this study were (1) to evaluate FDG PET/CT and CT for the detection of axillary lymph node metastases in breast cancer (BC) patients and (2) to evaluate FDG PET/CT as a pre-test for the triage to sentinel lymph node biopsy (SLNB) versus axillary lymph node dissection (ALND). METHODS:The sensitivity...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-009-1145-6
更新日期:2009-10-01 00:00:00
abstract:PURPOSE:We report the biodistribution and radiation dosimetry of an integrin αvβ3 specific PET tracer (18)F-AlF-NOTA-E[PEG4-c(RGDfk)]2) (denoted as (18)F-Alfatide II). We also assessed the value of (18)F-Alfatide II in patients with brain metastases. METHODS:A series of torso (from the skull to the thigh) static image...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-015-3118-2
更新日期:2015-12-01 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:It is a matter of controversy whether prophylactic lymph node dissection improves prognosis and survival in papillary thyroid carcinoma (PTC) patients without suspicion of lymph node metastases either clinically or on ultrasonography. It is possible that in such patients the use of lymphatic mapping and sentine...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-006-0316-y
更新日期:2007-06-01 00:00:00
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journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-012-2229-2
更新日期:2012-12-01 00:00:00
abstract::This proposal for standardization of (123)I-metaiodobenzylguanidine (iobenguane, MIBG) cardiac sympathetic imaging includes recommendations for patient information and preparation, radiopharmaceutical, injected activities and dosimetry, image acquisition, quality control, reconstruction methods, attenuation, scatter a...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章,实务指引
doi:10.1007/s00259-010-1491-4
更新日期:2010-08-01 00:00:00
abstract:PURPOSE:Several patients experience unexplained persistent symptoms after SARS-CoV-2 recovering. We aimed at evaluating if 2-deoxy-2-[18F]fluoro-D-glucose ([18F]FDG) was able to demonstrate a persistent inflammatory process. METHODS:Recovered adult COVID-19 patients, who complained unexplained persisting symptoms for ...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-020-05084-3
更新日期:2020-10-30 00:00:00
abstract:PURPOSE:Vascular stiffness may potentially be used as a screening tool to identify asymptomatic patients with diabetes with abnormal myocardial perfusion. The purpose of this study was therefore to determine the association between vascular stiffness, measured in term of pulse wave velocity (PWV) and augmentation index...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 临床试验,杂志文章
doi:10.1007/s00259-011-1894-x
更新日期:2011-11-01 00:00:00
abstract:OBJECTIVE:The pattern expression score (PES), i.e., the degree to which a pathology-related pattern is present, is frequently used in FDG-brain-PET analysis and has been shown to be a powerful predictor of conversion to Alzheimer's disease (AD) in mild cognitive impairment (MCI). Since, inevitably, the PES is affected ...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章,多中心研究
doi:10.1007/s00259-019-04400-w
更新日期:2019-10-01 00:00:00
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journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-009-1356-x
更新日期:2010-05-01 00:00:00
abstract:PURPOSE:Our aim was to assess the prognostic and predictive value of somatostatin receptor 2 (sstr2) in neuroendocrine tumors (NETs). METHODS:We established a tissue microarray and imaging database from NET patients that received sstr2-targeted radiopeptide therapy with yttrium-90-DOTATOC, lutetium-177-DOTATOC or alte...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-016-3486-2
更新日期:2017-03-01 00:00:00
abstract::Chronic cigarette smoking alters coronary vascular endothelial response. To determine whether altered response also occurs in young individuals without manifest coronary disease we quantified coronary blood flow at rest, following adenosine vasodilator stress and during the cold pressor test in healthy young smokers. ...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 临床试验,杂志文章
doi:10.1007/s00259-002-0818-1
更新日期:2002-08-01 00:00:00
abstract::We assessed the accuracy of brain perfusion single-photon emission computed tomography (SPECT) in discriminating between patients with probable Alzheimer's disease (AD) at the very early stage and age-matched controls before and after partial volume correction (PVC). Three-dimensional MRI was used for PVC. We randomly...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/s00259-004-1491-3
更新日期:2004-07-01 00:00:00
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journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-020-05128-8
更新日期:2021-01-08 00:00:00
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journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-002-0858-6
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abstract:INTRODUCTION:Ischemia in hypertrophic cardiomyopathy (HCM) is caused by coronary microvascular dysfunction (CMD), which is detected by measuring myocardial blood flow (MBF) with PET. Whether CMD may be associated with ischemic left ventricular (LV) dysfunction is unclear. We therefore assessed LV ejection fraction (EF)...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
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更新日期:2017-05-01 00:00:00
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journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
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更新日期:2009-10-01 00:00:00
abstract:PURPOSE:PSMA ligand imaging with hybrid PET/MRI scanners could be an integral part of the clinical routine in the future. However, the first study about this novel method revealed a severe photopenic artifact ("halo artifact") around the urinary bladder causing significantly reduced tumor visibility. The aim of this ev...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-017-3718-0
更新日期:2017-09-01 00:00:00
abstract::As measurement of glomerular filtration rate (GFR) is now generally the responsibility of departments of nuclear medicine, it is important for nuclear medicine physicians and scientists to understand the pharmacokinetics of the indicators and radiotracers that are used, generally known as filtration markers. The singl...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章,评审
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更新日期:2004-01-01 00:00:00
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journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-009-1143-8
更新日期:2009-10-01 00:00:00
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journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章,评审
doi:10.1007/s00259-005-1856-2
更新日期:2005-11-01 00:00:00
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journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 临床试验,杂志文章
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更新日期:2002-07-01 00:00:00
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journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-005-1955-0
更新日期:2006-03-01 00:00:00
abstract:PURPOSE:Positron emission tomography (PET) radioligands specific to α7 nicotinic acetylcholine receptors (nAChRs) afford in vivo imaging of this receptor for neuropathologies such as Alzheimer's disease, schizophrenia, and substance abuse. This work aims to characterize the kinetic properties of an α7-nAChR-specific ra...
journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-015-3209-0
更新日期:2016-03-01 00:00:00
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journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-020-04854-3
更新日期:2020-08-01 00:00:00
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journal_title:European journal of nuclear medicine and molecular imaging
pub_type: 杂志文章
doi:10.1007/s00259-006-0198-z
更新日期:2007-03-01 00:00:00