1210. Bifeprunox
Nomenclature
CAS number: 350992-10-8
7-[4-([1,1′-Biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone. C24H23N3O2; mol wt 385.46.
C 74.78%, H 6.01%, N 10.90%, O 8.30%.
Description and references
Exhibits partial agonist activity at dopamine D2 and serotonin 5-HT1A receptors. Prepn: R. W. Feenstra et al., WO 9736893; eidem, US 6225312 (1997, 2001 both to Duphar); and receptor binding studies: idem et al., Bioorg. Med. Chem. Lett. 11, 2345 (2001). Analysis of binding affinity vs in vitro efficacy: A. Newman-Tancredi et al., Int. J. Neuropsychopharmacol. 8, 341 (2005). Review of development: W. Wolf, Curr. Opin. Investig. Drugs 4, 72-76 (2003).
Derivative
Methanesulfonate.Nomenclature
CAS number: 350992-13-1
Bifeprunox mesylate; DU-127090. C24H23N3O2.CH4O3S; mol wt 481.56.
C 62.35%, H 5.65%, N 8.73%, O 16.61%, S 6.66%.
Therapeutic Category
Antipsychotic.
Keywords
Antipsychotic; Dopamine-Serotonin System Stabilizer