F17464

F17464 is a novel small molecule antipsychotic developed by Pierre Fabre. It acts as a highly selective dopamine D3 receptor antagonist (with approximately 70-fold selectivity over D2 receptors) and also functions as a partial agonist at the serotonin 5-HT1A receptor. The compound demonstrates high affinity for human dopamine D3 (Ki = 0.17 nM) and serotonin 5-HT1A (Ki = 0.16 nM) receptors, with much lower affinity for dopamine D2 short and long forms (Ki = 8.9 and 12.1 nM). Preclinical studies show that F17464 blocks ketamine-induced morphological changes in dopaminergic neurons via the D3 receptor, increases dopamine release in the prefrontal cortex and striatum, reduces MK801-induced c-fos mRNA expression changes, and rescues social interaction deficits in animal models of autism. In clinical trials for acute schizophrenia, F17464 demonstrated efficacy in reducing psychotic symptoms with a favorable safety profile—showing no significant weight gain or extrapyramidal side effects[1][2][3][6][8].