title: Imaging the dopamine uptake site with ex vivo [18F]GBR 13119 binding autoradiography in rat brain.
abstract: We studied the binding of [18F]GBR 13119 (1-[[(4-[18F]fluorophenyl) (phenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine) to rat brain with autoradiography after intravenous injection. The rank order of binding was dorsal striatum greater than nucleus accumbens = olfactory tubercle greater than substantia nigra = ventral tegmental area greater than other areas. Binding was blocked by prior injection of dopamine uptake blockers but not by injection of dopamine receptor antagonists or drugs that bind to the dialkylpiperazine site. Unilateral 6-hydroxy-dopamine lesions of dopamine neurons caused a marked decrease in striatal and nigral binding on the side of the lesion. We conclude that intravenous injection of [18F]GBR 13119 provides a useful marker of presynaptic dopamine uptake sites.
authors.affiliation: Department of Neurology, University of Michigan, Ann Arbor 48104-1687.
authors.forename: B J
authors.initials: BJ
authors.lastname: Ciliax
authors.forename: M R
authors.initials: MR
authors.lastname: Kilbourn
authors.forename: M S
authors.initials: MS
authors.lastname: Haka
authors.forename: J B
authors.initials: JB
authors.lastname: Penney
mesh_terms: D000818:Animals; D001345:Autoradiography; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D002531:Cerebellum / Q000378:metabolism; D002540:Cerebral Cortex / Q000378:metabolism; D003342:Corpus Striatum / Q000378:metabolism; D004298:Dopamine / Q000378:metabolism*; D006892:Hydroxydopamines / Q000494:pharmacology; D008024:Ligands; D008297:Male; D009627:Nomifensine / Q000494:pharmacology; D009714:Nucleus Accumbens / Q000378:metabolism; D009830:Olfactory Bulb / Q000378:metabolism; D016627:Oxidopamine; D010879:Piperazines / Q000378:metabolism* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013681:Tegmentum Mesencephali / Q000378:metabolism; D014018:Tissue Distribution
chemical_list: D006892:Hydroxydopamines; D008024:Ligands; D010879:Piperazines; D009627:Nomifensine; C055278:GBR 13119; D016627:Oxidopamine; D004298:Dopamine