title: Synthesis of [11C]RPR-72840A and its evaluation as a radioligand for the serotonin reuptake site in positron emission tomography.
abstract: RPR-72840A, an inhibitor of serotonin reuptake, was labelled with carbon-11. The synthesis of the nonradioactive precursor, which exhibited some unexpected chemistry, and its reaction with [11C]phosgene affording [11C]RPR-72840A are described. Biodistribution studies in rats and PET studies in baboons were conducted to evaluate [11C]RPR-72840A as a tracer for PET imaging of the serotonin reuptake system.
authors.affiliation: CEA, Service Hospitalier Frédéric Joliot, Orsay, France. ROEDA@DSVIDF.CEA.FR
authors.forename: D
authors.initials: D
authors.lastname: Roeda
authors.forename: B
authors.initials: B
authors.lastname: Tavitian
authors.forename: C
authors.initials: C
authors.lastname: Coulon
authors.forename: F
authors.initials: F
authors.lastname: David
authors.forename: F
authors.initials: F
authors.lastname: Dollé
authors.forename: C
authors.initials: C
authors.lastname: Fuseau
authors.forename: A
authors.initials: A
authors.lastname: Jobert
authors.forename: C
authors.initials: C
authors.lastname: Crouzel
mesh_terms: D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D002250:Carbon Radioisotopes; D005069:Evaluation Studies as Topic; D008297:Male; D010215:Papio; D011799:Quinazolines / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D012701:Serotonin / Q000378:metabolism*; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed
chemical_list: D002250:Carbon Radioisotopes; D011799:Quinazolines; D012701:Serotonin; D017367:Selective Serotonin Reuptake Inhibitors; C105914:RPR 72840A