In vivo binding of [18F]GBR 13119 to the brain dopamine uptake system.
Regional rat brain uptake of [18F]GBR 13119, a high specific activity, positron-emitter labeled derivative of the potent dopamine uptake antagonist GBR 12935, is reported. Striatum to cerebellum ratios of 3 are obtained at 90 minutes post injection. Specific binding in striatum can be blocked by pretreatment with dopamine uptake system antagonists (mazindol, nomifensine) but not with receptor antagonists (spiperone, flupenthixol). [18F]GBR 13119 is proposed as a new positron-emitting radioligand for in vivo PET studies of the pre-synaptic dopamine uptake system.
Kilbourn
M R
MR
Department of Internal Medicine, University of Michigan Medical Center, Ann Arbor 48109.
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D002531:Cerebellum / Q000187:drug effects / Q000378:metabolism; D002540:Cerebral Cortex / Q000378:metabolism; D003342:Corpus Striatum / Q000187:drug effects / Q000378:metabolism; D004298:Dopamine / Q000378:metabolism*; D005475:Flupenthixol / Q000494:pharmacology; D007700:Kinetics; D008454:Mazindol / Q000494:pharmacology; D009627:Nomifensine / Q000494:pharmacology; D010879:Piperazines / Q000493:pharmacokinetics*; D051381:Rats; D011919:Rats, Inbred Strains; D013134:Spiperone / Q000494:pharmacology
D010879:Piperazines; D009627:Nomifensine; D013134:Spiperone; C055278:GBR 13119; D008454:Mazindol; D005475:Flupenthixol; D004298:Dopamine