title: PET-characterization of [carbonyl-11C]WAY-100635 binding to 5-HT1A receptors in the primate brain.
abstract: [carbonyl-11C]WAY-100635 is a new radioligand which can be used with positron emission tomography (PET) to provide high contrast delineation of human brain regions that are rich in 5-HT1A receptors. In the present PET study, the binding of [carbonyl-11C]WAY-100635 was characterized in the cynomolgus monkey brain. Pretreatment with each of the two reference compounds, WAY-100635 and 8-OH-DPAT, as well as the drugs buspirone and pindolo, induced a marked inhibition of [carbonyl-11C]WAY-100635 binding in the neocortex and the raphe nuclei. A preliminary Scatchard analysis yielded 5-HT1A receptor density values of the same order as those that have been reported in vitro. The study shows that [carbonyl-11C]WAY-100635 binds specifically to 5-HT1A receptors in the primate brain and has potential for determination of 5-HT1A receptor occupancy and density in psychiatric patients.
authors.affiliation: Department of Clinical Neuroscience, Karolinska Institute, Stockholm, Sweden. lars.fard.@neuro.ks.se
authors.forename: L
authors.initials: L
authors.lastname: Farde
authors.forename: N
authors.initials: N
authors.lastname: Ginovart
authors.forename: H
authors.initials: H
authors.lastname: Ito
authors.forename: C
authors.initials: C
authors.lastname: Lundkvist
authors.forename: V W
authors.initials: VW
authors.lastname: Pike
authors.forename: J A
authors.initials: JA
authors.lastname: McCarron
authors.forename: C
authors.initials: C
authors.lastname: Halldin
mesh_terms: D017371:8-Hydroxy-2-(di-n-propylamino)tetralin / Q000378:metabolism; D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D002065:Buspirone / Q000378:metabolism; D002250:Carbon Radioisotopes; D002531:Cerebellum / Q000378:metabolism; D008252:Macaca fascicularis; D008297:Male; D019579:Neocortex / Q000378:metabolism; D010869:Pindolol / Q000378:metabolism; D010879:Piperazines / Q000378:metabolism*; D011725:Pyridines / Q000378:metabolism*; D011903:Raphe Nuclei / Q000378:metabolism; D011985:Receptors, Serotonin / Q000378:metabolism*; D044263:Receptors, Serotonin, 5-HT1; D014055:Tomography, Emission-Computed
chemical_list: D002250:Carbon Radioisotopes; D010879:Piperazines; D011725:Pyridines; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; C090413:N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D010869:Pindolol; D002065:Buspirone