In vivo labeling of cocaine binding sites on dopamine transporters with [3H]WIN 35,428.
After in vivo administration, [3H]WIN 35,428 accumulated in mouse brain regions containing dopaminergic nerve terminals. The highest accumulation was in the striatum and it peaked between 30 and 60 min. The accumulation was saturable with increasing doses of WIN 35,428, and was blocked by compounds that bind to the dopamine transporter. Paroxetine, a drug that blocks serotonin transporters, had no effect. Moreover, the in vivo potency of cocaine analogs correlated with their in vitro potency. Thus, [3H]WIN 35,428 is a suitable ligand for labeling cocaine receptors associated with dopamine transporters in vivo.
Scheffel
U
U
Department of Radiology, Johns Hopkins Medical Institutions, Baltimore, Maryland.
Pögün
S
S
Stathis
M
M
Boja
J W
JW
Kuhar
M J
MJ
D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D002352:Carrier Proteins / Q000378:metabolism*; D002531:Cerebellum / Q000378:metabolism; D003042:Cocaine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000493:pharmacokinetics; D003342:Corpus Striatum / Q000378:metabolism; D050483:Dopamine Plasma Membrane Transport Proteins; D066298:In Vitro Techniques; D008297:Male; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D051379:Mice; D008815:Mice, Inbred Strains; D009419:Nerve Tissue Proteins; D011869:Radioligand Assay; D011955:Receptors, Drug / Q000187:drug effects / Q000378:metabolism*; D014018:Tissue Distribution
D002352:Carrier Proteins; D050483:Dopamine Plasma Membrane Transport Proteins; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D011955:Receptors, Drug; C061445:cocaine receptor; C021279:(1R-(exo,exo))-3-(4-fluorophenyl)-8-methyl-8- azabicyclo(3.2.1)octane-2-carboxylic acid, methyl ester; D003042:Cocaine