PMID: 2573104Jan 1, 1989Paper

D1- and D2-dopamine receptor occupancy during treatment with conventional and atypical neuroleptics

Psychopharmacology
L FardeG Sedvall

Abstract

Using positron emission tomography and the selective ligands 11C-SCH23390 and 11C-raclopride, central D1- and D2-dopamine receptor occupancy was determined in schizophrenic patients treated with clinical doses of classical and atypical neuroleptics. Treatment with ten chemically distinct classical neuroleptics resulted in a 65-89% occupancy of D2-dopamine receptors. This finding represents strong support for the hypothesis that the mechanism of action of antipsychotic drugs is indeed related to a substantial degree of D2-dopamine receptor occupancy. In two patients treated with the atypical neuroleptic clozapine, 300 mg b.i.d. and 150 mg b.i.d., the D2-dopamine receptor occupancy was 65 and 40%, respectively. D1-dopamine receptor occupancy was determined in six antipsychotic drug-treated patients. No D1-dopamine receptor occupancy was found in patients treated with sulpiride and perphenazine, compounds known to be selective D2-dopamine receptor antagonists. The highest D1-dopamine receptor occupancy, 42%, was found in the patient treated with clozapine 150 mg b.i.d. The effects of the atypical neuroleptic clozapine may be related to a combined effect on both D1- and D2-dopamine receptors.

References

Feb 1, 1978·The American Journal of Psychiatry·A Carlsson
Jan 11, 1979·Nature·J W Kebabian, D B Calne
Sep 1, 1985·Archives of General Psychiatry·T R Barnes, W M Braude
Jan 14, 1986·European Journal of Pharmacology·P H AndersenC Braestrup
Jul 1, 1987·Archives of General Psychiatry·L FardeG Sedvall
Oct 1, 1986·Archives of General Psychiatry·G SedvallF A Wiesel
Jan 1, 1986·International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes·C HalldinG Sedvall
Jul 15, 1983·European Journal of Pharmacology·J Hyttel

❮ Previous
Next ❯

Citations

Jan 1, 1992·The Psychiatric Quarterly·J A Lieberman, A Z Safferman
Jan 1, 1995·Journal of Neural Transmission. General Section·I KusumiT Koyama
Mar 1, 1996·Psychopharmacology·B J Kinon, J A Lieberman
Mar 28, 2008·Neurotoxicity Research·Márcio R MartinsJoão Quevedo
Jan 12, 2012·Psychopharmacology·Philippe CorbeilEmmanuelle Pourcher
Oct 24, 2012·Psychopharmacology·Akihiro TakanoLars Farde
Mar 21, 2009·European Journal of Nuclear Medicine and Molecular Imaging·Akihiro TakanoChrister Halldin
Aug 16, 2005·Current Psychiatry Reports·Thomas W Weickert, Terry E Goldberg
Aug 14, 1992·European Journal of Pharmacology·P H AndersenE B Nielsen
Oct 20, 1992·European Journal of Pharmacology·S L Mason, G P Reynolds
Jul 1, 1992·Pharmacology, Biochemistry, and Behavior·E A LohD C Roberts
May 1, 1993·Pharmacology, Biochemistry, and Behavior·C MarinT N Chase
Jan 1, 1996·Neuroscience and Biobehavioral Reviews·M L Wadenberg
Feb 1, 1993·Psychiatry Research·A I GreenJ J Schildkraut
Mar 1, 1992·Neurochemistry International·H HallG Sedvall
Jan 1, 1992·Progress in Neuro-psychopharmacology & Biological Psychiatry·M R Lynch
Feb 17, 1992·Neuroscience Letters·M Mercugliano, M F Chesselet

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antipsychotic Drugs

Antipsychotic drugs are a class of medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia and bipolar disorder. Discover the latest research on antipsychotic drugs here