D1- and D2-dopamine receptor occupancy during treatment with conventional and atypical neuroleptics.
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Farde L, Wiesel FA, Nordstrom AL, Sedvall G
D1- and D2-dopamine receptor occupancy during treatment with conventional and atypical neuroleptics.
Psychopharmacology (Berl). 1989;99 Suppl:S28-31.
- PubMed ID
- 2573104 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Perphenazine Dopamine D1 receptor Protein Humans YesAntagonistDetails Perphenazine Dopamine D2 receptor Protein Humans YesAntagonistDetails