Downregulation of 5-HT7 serotonin receptors by the atypical antipsychotics clozapine and olanzapine: role of motifs in the C-terminal domain and interaction with GASP-1 Universiteit Gent
The human 5-HT7 serotonin receptor, a G-protein-coupled receptor (GPCR), activates adenylyl cyclase constitutively and upon agonist activation. Biased ligands differentially activate 5-HT7 serotonin receptor desensitization, internalization and degradation in addition to G protein activation. We have previously found that the atypical antipsychotics clozapine and olanzapine inhibited G protein Lysosome activation and, surprisingly, induced both ...