Supriya A Gaitonde, Charlotte Avet, Mario de la Fuente Revenga, Elodie Blondel-Tepaz, Aida Shahraki, Adrian Morales Pastor, Valerij Talagayev, Patricia Robledo, Peter Kolb, Jana Selent, Javier González-Maeso, Michel Bouvier
The intricate involvement of the serotonin 5-HT2A receptor (5-HT2A R) both in schizophrenia and in the activity of antipsychotic drugs is widely acknowledged. The currently marketed antipsychotic drugs, although effective in managing the symptoms of schizophrenia to a certain extent, are not without their repertoire of serious side effects. There is a need for better therapeutics to treat schizophrenia for which understanding the mechanism of action of the current antipsychotic drugs is imperative. With bioluminescence resonance energy transfer (BRET) assays, we trace the signaling signature of six antipsychotic drugs belonging to three generations at the 5-HT2A R for the entire spectrum of signaling pathways activated by serotonin (5-HT)...
April 2, 2024: Molecular Psychiatry