New data on the mechanism of action of antipsychotics

The 5-HT2A serotonin receptor is involved in both schizophrenia and the mode of action of antipsychotic drugs. While antipsychotic drugs have a certain efficacy in treating the symptoms of schizophrenia, they are associated with side effects, some of them major. To find out more about the mechanism of action of antipsychotic drugs, researchers have used bioluminescence resonance energy transfer (BRET) tests. They were able to work out the signaling signatures of six antipsychotic drugs, all acting on the 5-HT2A receptor. Risperidone, clozapine, olanzapine and haloperidol showed selective G-protein inverse agonist activity. In addition, selective partial G-protein agonism was observed for aripiprazole and cariprazine.