Skip to main content

Thank you for visiting You are using a browser version with limited support for CSS. To obtain the best experience, we recommend you use a more up to date browser (or turn off compatibility mode in Internet Explorer). In the meantime, to ensure continued support, we are displaying the site without styles and JavaScript.

Radioreceptor Binding Profile of the Atypical Antipsychotic Olanzapine


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.

Author information



Corresponding author

Correspondence to Frank P Bymaster MS.

Rights and permissions

Reprints 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).

Download citation


  • Olanzapine
  • Clozapine
  • Haloperidol
  • Antipsychotic
  • Binding profile
  • Dopamine
  • Risperidone
  • Seroquel
  • Org 5222

Further reading


Quick links