Psychopharmacology

, Volume 103, Issue 2, pp 150–153 | Cite as

11C-SCH 39166, a selective ligand for visualization of dopamine-D1 receptor binding in the monkey brain using PET

  • Göran Sedvall
  • Lars Farde
  • Allen Barnett
  • Håkan Hall
  • Christer Halldin
Original Investigations
Received:
Revised:

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.

Key words

D1-dopamine receptors Positron emission tomography Monkey brain Dopamine receptor antagonist Antipsychotic drugs 
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References

  1. 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 15–25Google Scholar
  2. 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 35:1885–1893Google Scholar
  3. 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 147:73–82Google Scholar
  4. 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 247:1093–1102Google Scholar
  5. Farde L, Halldin C, Stone-Elander S, Sedvall G (1987) PET analysis of human dopamine receptor subtypes using11C-SCH 23390 and11C-raclopride. Psychopharmacology 92:278–284Google Scholar
  6. 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 73:7–21Google Scholar
  7. 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 37:1039–1043Google Scholar
  8. 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 31:737Google Scholar
  9. Holte S, Eriksson L, Dahlbom M (1989) A preliminary evaluation of the Scanditronix PC2048–15B brain scanner. Eur J Nucl Med 15:719–721Google Scholar
  10. Hyttel J (1983) SCH 23390 — the first selective dopamine D1-antagonist. Eur J Pharmacol 91:153–154Google Scholar
  11. 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 226:462–468Google Scholar
  12. Kebabian JW, Calne DB (1979) Multiple receptors for dopamine. Nature 277:93–96Google Scholar
  13. 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 119–124Google Scholar
  14. 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 43:1–52Google Scholar

Copyright information

© Springer-Verlag 1991

Authors and Affiliations

  • Göran Sedvall
    • 1
  • Lars Farde
    • 1
  • Allen Barnett
    • 2
  • Håkan Hall
    • 1
  • Christer Halldin
    • 1
  1. 1.Department of Psychiatry and PsychologyKarolinska InstituteStockholmSweden
  2. 2.Schering-Plough CorporationBloomfieldUSA

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