F-17464 is a dopamine D3 receptor antagonist and serotonin 5-HT1A receptor partial agonist which was under development for the treatment of schizophrenia but was never marketed. It is taken orally.
The drug's affinities (Ki) have been found to be 0.17nM for the dopamine D3 receptor, 0.16nM for the serotonin 5-HT1A receptor, and 8.9 to 12.1nM for the dopamine D2 receptor, with more than 50-fold selectivity for the dopamine D3 receptor over the dopamine D2 receptor. It also shows a much slower dissociation rate from the dopamine D3 receptor than from the dopamine D2 receptor. The drug possesses low affinity for the serotonin 5-HT2A and 5-HT2C receptors (Ki = 437nM and 1,995nM, respectively). F-17464 showed more than 80% occupancy of the dopamine D3 receptor and only 20% occupancy of the dopamine D2 receptor with positron emission tomography (PET) imaging in humans. It inhibited amphetamine- and dizocilpine (MK-801)-induced hyperlocomotion in rodents.
F-17464 was first described in the scientific literature by 2015. It was under development by Pierre Fabre. The drug reached phase 2 clinical trials for schizophrenia prior to the discontinuation of its development in 2021. The findings of a phase 2 trial have been published.
See also List of investigational antipsychotics
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