title: Synthesis and characterization of a iodine-125-labeled pyrrolo[1,2-a]thieno[3,2-e]pyrazine and evaluation as a potential 5-HT4R SPECT tracer.
abstract: In the aim to find new radiotracers for the in vivo imaging of 5-HT(4) receptors by ultra-high resolution quantitative SPECT, we have developed the synthesis of a radioiodinated 5-HT(4) ligand using an iododestannylation procedure. The [(125)I]-ligand was obtained in a high radiochemical yield. Preliminary autoradiographic and ex vivo studies failed to show a specific labeling of 5-HT(4) receptors.
authors.affiliation: Centre d'Etudes et de Recherche sur le Médicament de Normandie, UPRES EA 4258, INC3M FR-CNRS 3038, UFR des Sciences Pharmaceutiques, Université de Caen Basse-Normandie, boulevard Becquerel 14032 Caen cedex, France.
authors.forename: Thomas
authors.initials: T
authors.lastname: Cailly
authors.forename: Noé
authors.initials: N
authors.lastname: Dumas
authors.forename: Philippe
authors.initials: P
authors.lastname: Millet
authors.forename: Stéphane
authors.initials: S
authors.lastname: Lemaître
authors.forename: Frédéric
authors.initials: F
authors.lastname: Fabis
authors.forename: Yves
authors.initials: Y
authors.lastname: Charnay
authors.forename: Sylvain
authors.initials: S
authors.lastname: Rault
mesh_terms: D002851:Chromatography, High Pressure Liquid; D007457:Iodine Radioisotopes / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D011719:Pyrazines / Q000138:chemical synthesis*; D011758:Pyrroles / Q000138:chemical synthesis*; D013876:Thiophenes / Q000138:chemical synthesis*; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: D007457:Iodine Radioisotopes; D011719:Pyrazines; D011758:Pyrroles; D013876:Thiophenes