Chemistry:F-17464

From HandWiki

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.[1][2][3][4][5][6] It is taken orally.[1]

The drug's affinities (Ki) have been found to be 0.17 nM for the dopamine D3 receptor, 0.16 nM for the serotonin 5-HT1A receptor, and 8.9 to 12.1 nM for the dopamine D2 receptor, with more than 50-fold selectivity for the dopamine D3 receptor over the dopamine D2 receptor.[6][3][5] It also shows a much slower dissociation rate from the dopamine D3 receptor than from the dopamine D2 receptor.[5] The drug possesses low affinity for the serotonin 5-HT2A and 5-HT2C receptors (Ki = 437 nM and 1,995 nM, respectively).[3] 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.[3][6][4][7] It inhibited amphetamine- and dizocilpine (MK-801)-induced hyperlocomotion in rodents.[4]

F-17464 was first described in the scientific literature by 2015.[8] It was under development by Pierre Fabre.[1][2] The drug reached phase 2 clinical trials for schizophrenia prior to the discontinuation of its development in 2021.[1][2] The findings of a phase 2 trial have been published.[6][3][9]

See also

References

  1. ↑ 1.0 1.1 1.2 1.3 "F 17464". 27 September 2021. https://adisinsight.springer.com/drugs/800036859. 
  2. ↑ 2.0 2.1 2.2 "Delving into the Latest Updates on F-17464 with Synapse". 28 March 2026. https://synapse.patsnap.com/drug/39361b311082467caa677c74f052529c. 
  3. ↑ 3.0 3.1 3.2 3.3 3.4 "New and emerging treatments for schizophrenia: a narrative review of their pharmacology, efficacy and side effect profile relative to established antipsychotics". Neuroscience and Biobehavioral Reviews 132: 324–361. January 2022. doi:10.1016/j.neubiorev.2021.11.032. PMID 34838528. 
  4. ↑ 4.0 4.1 4.2 "The dopamine D3 receptor, a quarter century later". The European Journal of Neuroscience 45 (1): 2–19. January 2017. doi:10.1111/ejn.13390. PMID 27600596. 
  5. ↑ 5.0 5.1 5.2 "Pharmacology profile of F17464, a dopamine D3 receptor preferential antagonist". European Journal of Pharmacology 890. January 2021. doi:10.1016/j.ejphar.2020.173635. PMID 33065094. 
  6. ↑ 6.0 6.1 6.2 6.3 "Unlocking the potential of lumateperone and novel anti-psychotics for schizophrenia". BioImpacts 15. 2025. doi:10.34172/bi.30259. PMID 40161932. 
  7. ↑ "Binding of the D3-preferring antipsychotic candidate F17464 to dopamine D3 and D2 receptors: a PET study in healthy subjects with [11C]-(+)-PHNO". Psychopharmacology (Berl) 237 (2): 519–527. February 2020. doi:10.1007/s00213-019-05387-w. PMID 31773210. 
  8. ↑ Joussot J (24 April 2015). Stratégies de synthèse d'un nouvel antipsychotique potentiel : cascades réactionnelles palladocatalysées : un outil puissant pour la synthèse de structures polycycliques complexes et hautement fonctionnalisées (phdthesis thesis) (in français). Université de Strasbourg. Retrieved 9 June 2026.
  9. ↑ "Randomized, double-blind, placebo-controlled study of F17464, a preferential D3 antagonist, in the treatment of acute exacerbation of schizophrenia". Neuropsychopharmacology 44 (11): 1917–1924. October 2019. doi:10.1038/s41386-019-0355-2. PMID 30822774. 

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