title: 2-[18F]Fluoro-A-85380, an in vivo tracer for the nicotinic acetylcholine receptors.
abstract: The in vivo brain regional distribution of 2-[18F]fluoro-A-85380, a novel tracer for positron emission tomographic (PET) studies, followed the regional densities of brain nAChRs reported in the literature. Evidence of binding to nAChRs and high specificity of the binding in vivo was demonstrated by inhibition with nAChR selective ligands as well as with unlabeled 2-fluoro-A-85380. A preliminary toxicology study of the 2-fluoro-A-85380 showed a relatively low biological effect. 2-[18F]Fluoro-A-85380 holds promise as a useful radiotracer for imaging of nAChRs with PET.
authors.affiliation: Brain Imaging Center, Intramural Research Program, NIDA, Baltimore, MD 21224, USA.
authors.forename: A G
authors.initials: AG
authors.lastname: Horti
authors.forename: U
authors.initials: U
authors.lastname: Scheffel
authors.forename: A O
authors.initials: AO
authors.lastname: Koren
authors.forename: H T
authors.initials: HT
authors.lastname: Ravert
authors.forename: W B
authors.initials: WB
authors.lastname: Mathews
authors.forename: J L
authors.initials: JL
authors.lastname: Musachio
authors.forename: P A
authors.initials: PA
authors.lastname: Finley
authors.forename: E D
authors.initials: ED
authors.lastname: London
authors.forename: R F
authors.initials: RF
authors.lastname: Dannals
mesh_terms: D000818:Animals; D001384:Azetidines / Q000378:metabolism / Q000493:pharmacokinetics* / Q000633:toxicity; D001667:Binding, Competitive / Q000187:drug effects; D005462:Fluorine Radioisotopes; D007275:Injections, Intravenous; D008297:Male; D051379:Mice; D011978:Receptors, Nicotinic / Q000032:analysis / Q000378:metabolism*; D014018:Tissue Distribution
chemical_list: C104288:A 85380; D001384:Azetidines; D005462:Fluorine Radioisotopes; D011978:Receptors, Nicotinic