title: Synthesis and in vitro evaluation of oxindole derivatives as potential radioligands for 5-HT(7) receptor imaging with PET.
abstract: The most recently discovered serotonin (5-HT) receptor subtype, 5-HT(7), is considered to be associated with several CNS disorders. Noninvasive in vivo positron emission tomography (PET) studies of cerebral 5-HT(7) receptors could provide a significant advance in the understanding of the neurobiology and eventual dysfunctions of the 5-HT(7) receptor. To date, no appropriate 5-HT(7) receptor PET ligand has been developed. Here, we modified known 5-HT(7) selective phenylpiperazinyl-butyloxindole derivatives so that they may be labeled either with carbon-11 or fluorine-18. A set of potential 5-HT(7) ligands for PET molecular imaging was successfully synthesized. Two compounds (10 and 14) were tested against a range of targets. Both compounds display a promising in vitro profile with respect to PET imaging of the 5-HT(7) receptor in thalamic regions.
authors.forename: Matthias M
authors.initials: MM
authors.lastname: Herth
authors.forename: Balázs
authors.initials: B
authors.lastname: Volk
authors.forename: Katalin
authors.initials: K
authors.lastname: Pallagi
authors.forename: Lasse
authors.initials: L
authors.lastname: Kofoed Bech
authors.forename: Ferenc A
authors.initials: FA
authors.lastname: Antoni
authors.forename: Gitte M
authors.initials: GM
authors.lastname: Knudsen
authors.forename: Jesper L
authors.initials: JL
authors.lastname: Kristensen
mesh_terms: D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism; D010880:Piperidines / Q000138:chemical synthesis*; D049268:Positron-Emission Tomography / Q000379:methods*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D011985:Receptors, Serotonin / Q000378:metabolism*
chemical_list: D010880:Piperidines; D019275:Radiopharmaceuticals; D011985:Receptors, Serotonin; C104425:serotonin 7 receptor