Abstract
The new selective D1-dopamine receptor antagonist SCH 39166 was labelled with the positron emitting isotope11C 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.
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References
Barnett A, Iorio LC, Billard W (1986) Relationship of the behavioral effects of SCH 23390 and related benzazepines to their effects on dopamine1 (D1) receptors. In: Biggio G, Spano PF, Gessa GL (eds) Modulation of central and peripheral neurotransmitter function. Liviana Press, Padova, Italy, pp 15–25
Billard W, Rupert V, Crosby G, Iorio LC, Barnett A (1984) Characterization of the binding of3H-SCH 23390, a selective D1-receptor antagonist ligand in rat striatum. Life Sci 35:1885–1893
Blin J, Pappata S, Kiyosawa M, Crouzel C, Baron JC (1988) [18F] Setoperone: a new high-affinity ligand for positron emission tomography study of the serotonin-2 receptors in baboon brain in vivo. Eur J Pharmacol 147:73–82
Chipkin RE, Iorio LC, Coffin VL, McQuade RD, Berger JG, Barnett A (1988) Pharmacological profile of SCH 39166: a dopamine-D1 selective benzonaphtazepine with potential antipsychotic activity. J Pharmacol Exp Ther 247:1093–1102
Farde L, Halldin C, Stone-Elander S, Sedvall G (1987) PET analysis of human dopamine receptor subtypes using11C-SCH 23390 and11C-raclopride. Psychopharmacology 92:278–284
Hall H, Farde L, Sedvall G (1988) Human dopamine receptor subtypes — in vitro binding analysis using 3H-SCH 23390 and 3H-raclopride. J Neural Transm 73:7–21
Halldin C, Stone-Elander S, Farde L, Ehrin E, Fasth K-J, Långström B, Sedvall G (1986) Preparation of11C-labelled SCH 23390 for the in vivo study of dopamine D1 receptors using positron emission tomography. Appl Radiat Isotopes 37:1039–1043
Halldin C, Farde L, Barnett A, Sedvall G (1990) Preparation of (11C)SCH 39166, a new selective D1-dopamine receptor ligand for PET. J Nucl Med 31:737
Holte S, Eriksson L, Dahlbom M (1989) A preliminary evaluation of the Scanditronix PC2048–15B brain scanner. Eur J Nucl Med 15:719–721
Hyttel J (1983) SCH 23390 — the first selective dopamine D1-antagonist. Eur J Pharmacol 91:153–154
Iorio LC, Barnett A, Leitz FH, Houser VP, Korduba CA (1983) SCH 23390, a potential benzazepine antipsychotic with unique interactions on dopaminergic systems. J Pharmacol Exp Ther 226:462–468
Kebabian JW, Calne DB (1979) Multiple receptors for dopamine. Nature 277:93–96
Sedvall G, Farde L, Stone-Elander S, Halldin C (1986) Dopamine D1-receptor binding in the living human brain. In: Breese GR Creese I (eds) Advances in experimental medicine and biology. Neurobiology of central D1-dopamine receptors, Vol 204. Plenum Press, New York, pp 119–124
Waddington JL, Boyle KM (1989) Drugs acting on brain dopamine receptors: a conceptual re-evaluation 5 years after the first selective D1 antagonist. Pharmacol Ther 43:1–52
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Sedvall, G., Farde, L., Barnett, A. et al. 11C-SCH 39166, a selective ligand for visualization of dopamine-D1 receptor binding in the monkey brain using PET. Psychopharmacology 103, 150–153 (1991). https://doi.org/10.1007/BF02244195
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DOI: https://doi.org/10.1007/BF02244195