11C-SCH 39166, a selective ligand for visualization of dopamine-D1 receptor binding in the monkey brain using PET.
The new selective D1-dopamine receptor antagonist SCH 39166 was labelled with the positron emitting isotope 11C and used as ligand for visualization of dopamine-D1 receptor binding in Cynomolgus monkeys by PET. After intravenous administration of the ligand a marked uptake of radioactivity was recorded in the D1-dopamine receptor-rich striatum and neocortex but not in the dopamine receptor-poor cerebellum. The uptake of radioactivity in striatum and neocortex was markedly displaced after the intravenous injection of a high dose of the D1-dopamine receptor antagonist SCH 23390 but not after the 5-HT2 receptor antagonist ketanserine. 11C-SCH 39166 should be a useful tool to explore D1-dopamine receptor characteristics in the living human brain by PET.
Department of Psychiatry and Psychology, Karolinska Institute, Stockholm, Sweden.
G
G
Sedvall
L
L
Farde
A
A
Barnett
H
H
Hall
C
C
Halldin
D000818:Animals; D014150:Antipsychotic Agents; D001552:Benzazepines / Q000494:pharmacology; D001921:Brain / Q000033:anatomy & histology* / Q000378:metabolism; D001923:Brain Chemistry / Q000187:drug effects; D007650:Ketanserin / Q000494:pharmacology; D008024:Ligands; D008252:Macaca fascicularis; D008297:Male; D011954:Receptors, Dopamine / Q000187:drug effects / Q000378:metabolism*; D017447:Receptors, Dopamine D1; D014055:Tomography, Emission-Computed
D014150:Antipsychotic Agents; D001552:Benzazepines; D008024:Ligands; D011954:Receptors, Dopamine; D017447:Receptors, Dopamine D1; C058081:ecopipam; D007650:Ketanserin