High 5-HT2 receptor occupancy in clozapine treated patients demonstrated by PET
- 1 February 1993
- journal article
- Published by Springer Nature in Psychopharmacology
- Vol. 110 (3), 365-367
- https://doi.org/10.1007/bf02251294
Abstract
The clinical benefit of the atypical antipsychotic drug clozapine may be related to a combined effect on D2 and 5-HT2 receptors. To examine the basis for this hypothesis, positron emission tomography (PET) and the radioligand [11C]N-methylspiperone were used to determine cortical 5-HT2 receptor occupancy in three psychotic patients treated with 125 mg, 175mg and 200mg clozapine daily. The uptake of [11C]N-methylspiperone in the frontal cortex was very low compared to that in neuroleptic naive schizophrenic patients. 5-HT2 receptor occupancy calculated in the clozapine treated patients was 84%, 87% and 90%. The results show that clinical treatment with clozapine induces a high 5-HT2 receptor occupancy in psychotic patients at a low dose level.Keywords
This publication has 11 references indexed in Scilit:
- Positron Emission Tomographic Analysis of Central D1 and D2 Dopamine Receptor Occupancy in Patients Treated With Classical Neuroleptics and ClozapineArchives of General Psychiatry, 1992
- Evaluation of the Karolinska new positron camera system; the Scanditronix PC2048-15BIEEE Transactions on Nuclear Science, 1990
- Effects of acute and chronic treatments with clozapine and haloperidol on serotonin (5-HT2) and dopamine (D2) receptors in the rat brainBrain Research, 1989
- Clinical studies on the mechanism of action of clozapine: the dopamine-serotonin hypothesis of schizophreniaPsychopharmacology, 1989
- Clozapine for the Treatment-Resistant SchizophrenicArchives of General Psychiatry, 1988
- Stereoselective binding of 11C-raclopride in living human brain ? a search for extrastriatal central D2-dopamine receptors by PETPsychopharmacology, 1988
- In vivo binding of 3H-N-methylspiperone to dopamine and serotonin receptorsLife Sciences, 1987
- An improved synthesis of (3-N-[11C]methyl)spiperoneInternational Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes, 1986
- Important Issues in the Drug Treatment of SchizophreniaSchizophrenia Bulletin, 1980
- Antipsychotic Drugs, Neurotransmitters, and SchizophreniaAmerican Journal of Psychiatry, 1978