Abstract
The affinities of olanzapine, clozapine, haloperidol, and four potential antipsychotics were compared on binding to the neuronal receptors of a number of neurotransmitters. In both rat tissues and cell lines transfected with human receptors olanzapine had high affinity for dopamine D1, D2, D4, serotonin (5HT)2A, 5HT2C, 5HT3, α1-adrenergic, histamine H1, and five muscarinic receptor subtypes. Olanzapine had lower affinity for α2-adrenergic receptors and relatively low affinity for 5HT1 subtypes, GABAA, β-adrenergic receptors, and benzodiazepine binding sites. The receptor binding affinities for olanzapine was quite similar in tissues from rat and human brain. The binding profile of olanzapine was comparable to the atypical antipsychotic clozapine, while the binding profiles for haloperidol, resperidone, remoxipride, Org 5222, and seroquel were substantially different from that of clozapine. The receptor binding profile of olanzapine is consistent with the antidopaminergic, antiserotonergic, and antimuscarinic activity observed in animal models and predicts atypical antipsychotic activity in man.
Similar content being viewed by others
Article PDF
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Bymaster, F., Calligaro, D., Falcone, J. et al. Radioreceptor Binding Profile of the Atypical Antipsychotic Olanzapine. Neuropsychopharmacol 14, 87–96 (1996). https://doi.org/10.1016/0893-133X(94)00129-N
Received:
Revised:
Accepted:
Published:
Issue Date:
DOI: https://doi.org/10.1016/0893-133X(94)00129-N
Keywords
This article is cited by
-
G protein-coupled receptors in neurodegenerative diseases and psychiatric disorders
Signal Transduction and Targeted Therapy (2023)
-
Chronic treatment with D2-antagonist haloperidol leads to inhibitory/excitatory imbalance in striatal D1-neurons
Translational Psychiatry (2023)
-
Cost-effectiveness analysis of olanzapine in four-drug antiemetic therapy in Japanese patients treated with highly emetogenic cisplatin-containing chemotherapy
Journal of Pharmaceutical Health Care and Sciences (2022)
-
GABA-A receptor differences in schizophrenia: a positron emission tomography study using [11C]Ro154513
Molecular Psychiatry (2021)
-
Olanzapine for the prophylaxis and rescue of chemotherapy-induced nausea and vomiting: a systematic review, meta-analysis, cumulative meta-analysis and fragility assessment of the literature
Supportive Care in Cancer (2021)