In search of a serotonin 5-HT(7) radiotracer for positron emission tomography, we developed 1-[2-[(2S)-1-(phenylsulfonyl)pyrrolidin-2-yl]ethyl]piperidin-4-yl 4-fluorobenzoate. After labeling in good yield with fluorine-18 via nitro for fluorine exchange, preliminary biological experiments with autoradiographies failed to evidence any specific 5-HT(7) receptor delineation.
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http://dx.doi.org/10.1016/j.bmcl.2010.04.076 | DOI Listing |
Ann Nucl Med
February 2024
Pharmaceutical Sciences Research Center, Hemoglobinopathy Institute, Mazandaran University of Medical Sciences, Sari, Iran.
Background: The 5-hydroxytryptamine receptor (5-HTR) family includes seven classes of receptors. The 5-HTR is the newest member of this family and contributes to different physiological and pathological processes. As a pathology, glioblastoma multiform (GBM) overexpresses 5-HTR; hence, this study aims to develop radiolabeled aryl piperazine derivatives as 5-HTR imaging agents.
View Article and Find Full Text PDFMol Pharm
June 2021
Department of Radiopharmacy, Faculty of Pharmacy, Pharmaceutical Sciences Research Center, Mazandaran University of Medical Sciences, Sari, Iran.
With a poor prognosis, glioblastoma multiforme is the most aggressive tumor of the central nervous system in humans. The aim of this study was to develop novel tracers for the tumor targeting and imaging of overexpressed serotonin-7 receptors (5-HTRs) in U-87 MG glioma xenografted nude mice. Two phenylpiperazine derivatives named as and were designed, and the corresponding radiotracers Tc- and Tc- were synthesized in high radiochemical purity (>95%).
View Article and Find Full Text PDFJ Labelled Comp Radiopharm
February 2020
Neurobiology Research Unit and Center for Integrated Molecular Imaging, Copenhagen University Hospital, Rigshospitalet, Copenhagen, Denmark.
The serotonin 7 (5-HT ) receptor is suggested to be involved in a broad variety of CNS disorders, but very few in vivo tools exist to study this important target. Molecular imaging with positron emission tomography (PET) would enable an in vivo characterization of the 5-HT receptor. However, no clinical PET radiotracer exists for this receptor, and thus we aimed to develop such a tracer.
View Article and Find Full Text PDFNeurosci Biobehav Rev
September 2014
Medical Research Council, Clinical Sciences Centre, Institute of Clinical Sciences, Hammersmith Hospital Campus, Imperial College London, London W12 0NN, UK; Department of Psychosis Studies, Institute of Psychiatry, King's College London, London SE5 8AF, UK.
Serotonergic dysfunction is thought to contribute to the pathophysiology of schizophrenia but the evidence has not been systematically synthesised before. We therefore systematically reviewed postmortem and in vivo molecular imaging studies of serotonin function in schizophrenia. We identified fifty relevant studies investigating eight different serotonin receptor systems in a total of 684 patients and 675 controls.
View Article and Find Full Text PDFNucl Med Biol
April 2014
University Lyon 1, CNRS, Institute of Chemistry and Biochemistry (UMR 5246), Villeurbanne, France; CERMEP-Imagerie du Vivant, Lyon, France. Electronic address:
Introduction: The brain serotonin-7 receptor (5-HT7) is the most recently discovered serotonin receptor. It is targeted by several drug-candidates in psychopharmacology and neuropharmacology. In these fields, positron emission tomography (PET) is a molecular imaging modality offering great promise for accelerating the development process from preclinical discovery to clinical phases.
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