title: Syntheses, radiolabelings, and in vitro evaluations of fluorinated PET radioligands of 5-HT6 serotoninergic receptors.
abstract: The 5-HT6 receptors are potent therapeutic targets for psychiatric and neurological diseases (schizophrenia, Alzheimer's disease, etc.). However, with lack of specific radiopharmaceuticals, their pharmacology is still incomplete and their exploration is limited to animal models. In this context, we have designed a fluorinated PET radiotracer, [(18)F]2FNQ1P, that possesses a high affinity and selectivity for 5-HT6. In vitro PET autoradiographies in rat brain sections with this radiotracer were in accordance with the 5-HT6 distribution pattern.
authors.affiliation: Institute of Chemistry and Biochemistry (ICBMS-UMR CNRS 5246), University of Lyon, University Lyon 1, CNRS, 43 Boulevard du 11 Novembre 1918, 69622 Lyon, France.
authors.forename: Julie
authors.initials: J
authors.lastname: Colomb
authors.forename: Guillaume
authors.initials: G
authors.lastname: Becker
authors.forename: Sylvain
authors.initials: S
authors.lastname: Fieux
authors.forename: Luc
authors.initials: L
authors.lastname: Zimmer
authors.forename: Thierry
authors.initials: T
authors.lastname: Billard
mesh_terms: D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D066298:In Vitro Techniques; D049268:Positron-Emission Tomography; D011869:Radioligand Assay; D011985:Receptors, Serotonin / Q000737:chemistry / Q000378:metabolism*
chemical_list: D005462:Fluorine Radioisotopes; D011985:Receptors, Serotonin; C097216:serotonin 6 receptor