Occupancy of central neurotransmitter receptors by risperidone, clozapine and haloperidol, measured ex vivo by quantitative autoradiography

@article{Schotte1993OccupancyOC,
  title={Occupancy of central neurotransmitter receptors by risperidone, clozapine and haloperidol, measured ex vivo by quantitative autoradiography},
  author={Alain Schotte and Paul F. M. Janssen and Anton A Megens and Jos{\'e}e E. Leysen},
  journal={Brain Research},
  year={1993},
  volume={631},
  pages={191-202}
}
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding
Risperidone and its active metabolite 9-OH-risperidone were compared to reference antipsychotic drugs (haloperidol, pipamperone, fluspirilene, clozapine, zotepine) and compounds under development
Risperidone: regional effects in vivo on release and metabolism of dopamine and serotonin in the rat brain
TLDR
In contrast to the regionally rather homogenous activation of brain DA systems caused by risperidone, the drug was found to enhance brain 5-HT metabolism preferentially in the MPC, as indicated by the elevated extracellular concentration of 5-HIAA in this region.
Survey on the pharmacodynamics of the new antipsychotic risperidone
TLDR
Risperidone can be characterized as a potent D2 antagonist with predominant 5HT2 antagonistic activity and optimal pharmacokinetic properties.
In vitro receptor binding and in vivo receptor occupancy in rat and guinea pig brain: risperidone compared with antipsychotics hitherto used.
TLDR
The predominant 5-HT2A-receptor occupancy most likely underlies risperidone's beneficial effects on the negative symptoms of schizophrenia and an adequately low D2-receptors occupancy adds to the treatment of positive symptoms with a low liability of EPS.
Selective effects on prefrontal cortex serotonin by dopamine D3 receptor agonism: Interaction with low-dose haloperidol
  • M. R. Lynch
  • Psychology, Medicine
    Progress in Neuro-Psychopharmacology and Biological Psychiatry
  • 1997
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