title: Synthesis and evaluation of novel serotonin 4 receptor radiotracers for single photon emission computed tomography.
abstract: Despite its implication in several physiological and pathological processes the serotonin subtype-4 receptor (5-HT4R) has seen limited effort for the development of radiolabeling agent especially concerning single photon emission computed tomography (SPECT). Bearing an ester function, the available ligands are rapidly susceptible to hydrolysis which limits their use in vivo. In this study the synthesis of iodinated benzamide and ketone analogs were described. Their affinity for the 5-HT4R and their lipophilicity were evaluated and the most promising derivatives were evaluated ex vivo for their binding to the receptor and for their ability to displace the reference ligand [(125)I]-SB207710.
authors.affiliation: Normandie Univ, UNICAEN, CERMN, F-14032 Caen, France.
authors.forename: Julien
authors.initials: J
authors.lastname: Lalut
authors.affiliation: Hôpitaux Universitaires de Genève, Département de Santé Mentale et de Psychiatrie, Service de Psychiatrie Générale, Unité des Biomarqueurs de Vulnérabilité, Chemin du Petit-Bel-Air, 2, CH-1225 Genève, Switzerland.
authors.forename: Benjamin B
authors.initials: BB
authors.lastname: Tournier
authors.affiliation: Normandie Univ, UNICAEN, CERMN, F-14032 Caen, France.
authors.forename: Thomas
authors.initials: T
authors.lastname: Cailly
authors.affiliation: Normandie Univ, UNICAEN, CERMN, F-14032 Caen, France.
authors.forename: Cédric
authors.initials: C
authors.lastname: Lecoutey
authors.affiliation: Normandie Univ, UNICAEN, CERMN, F-14032 Caen, France.
authors.forename: Sophie
authors.initials: S
authors.lastname: Corvaisier
authors.affiliation: Normandie Univ, UNICAEN, CERMN, F-14032 Caen, France.
authors.forename: Audrey
authors.initials: A
authors.lastname: Davis
authors.affiliation: Normandie Univ, UNICAEN, CERMN, F-14032 Caen, France.
authors.forename: Céline
authors.initials: C
authors.lastname: Ballandonne
authors.affiliation: Normandie Univ, UNICAEN, CERMN, F-14032 Caen, France.
authors.forename: Marc
authors.initials: M
authors.lastname: Since
authors.affiliation: Hôpitaux Universitaires de Genève, Département de Santé Mentale et de Psychiatrie, Service de Psychiatrie Générale, Unité des Biomarqueurs de Vulnérabilité, Chemin du Petit-Bel-Air, 2, CH-1225 Genève, Switzerland.
authors.forename: Philippe
authors.initials: P
authors.lastname: Millet
authors.affiliation: Normandie Univ, UNICAEN, CERMN, F-14032 Caen, France.
authors.forename: Frédéric
authors.initials: F
authors.lastname: Fabis
authors.affiliation: Normandie Univ, UNICAEN, CERMN, F-14032 Caen, France.
authors.forename: Patrick
authors.initials: P
authors.lastname: Dallemagne
authors.affiliation: Normandie Univ, UNICAEN, CERMN, F-14032 Caen, France. Electronic address: christophe.rochais@unicaen.fr.
authors.forename: Christophe
authors.initials: C
authors.lastname: Rochais
mesh_terms: D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis* / Q000737:chemistry; D060326:Chemistry Techniques, Synthetic; D006801:Humans; D007457:Iodine Radioisotopes; D007659:Ketones / Q000138:chemical synthesis* / Q000737:chemistry; D011849:Radioactive Tracers; D051381:Rats; D017207:Rats, Sprague-Dawley; D044422:Receptors, Serotonin, 5-HT4 / Q000378:metabolism*; D015899:Tomography, Emission-Computed, Single-Photon / Q000379:methods*
chemical_list: D001549:Benzamides; D007457:Iodine Radioisotopes; D007659:Ketones; D011849:Radioactive Tracers; D044422:Receptors, Serotonin, 5-HT4; C037689:benzamide
keywords: 5-HT(4); Molecular imaging; Radioligand; SPECT; Serotonin