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}
}
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213 Citations
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213 Citations

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Risperidone: regional effects in vivo on release and metabolism of dopamine and serotonin in the rat brain

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.

Effect of clozapine and risperidone on 5-HT2 and D2-dopamine receptor binding in the post-mortem human brain. An autoradiographic study

Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine.

Survey on the pharmacodynamics of the new antipsychotic risperidone

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.

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.

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  • 1997

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Involvement of histamine receptors in the atypical antipsychotic profile of clozapine: a reassessment in vitro and in vivo

Clozapine and its active metabolite NDMC interact with the four human histamine receptors at clinically relevant concentrations, which may substantiate, at least in part, the atypical antipsychotic profile of clozapines, as well as its central and peripheral side effects such as sedation and weight gain.
...

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In vivo binding in rats, using intravenous administration of [3H]spiperone, and in vitro receptor binding and monoamine uptake inhibition profiles, revealed very potent occupation by ocaperidone and risperidone of 5HT2 receptors in the frontal cortex, which were 6, 30, and 100 times more potent than ritanserin, haloperidol, and clozapine.

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