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Bifeprunox


Bifeprunox
Systematic (IUPAC) name
7-[4-[(3-Phenylphenyl)methyl]piperazin-1-yl]-3H-benzooxazol-2-one
Identifiers
CAS number	?
ATC code	?
PubChem	208951
Chemical data
Formula	C₂₄H₂₃N₃O₂
Mol. mass	385.458 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	?

Bifeprunox is a novel atypical antipsychotic agent which, along with SLV313, aripiprazole and SSR-181507 combines minimal D₂ receptor agonism with 5-HT receptor agonism. ^[1]

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Bifeprunox has a novel mechanism of action. Conventional antipsychotics are classed into typical and atypical. The typical antipsychotics, such as chlorpromazine and haloperidol are potent D₂ receptor antagonists. The atypical antipsychotics started with clozapine, these are classified as multireceptor interacting compounds, acting as an agonist towards 5-HT_1A and an antagonist towards D₂ receptors among other 5-HT and DA receptors. Bifeprunox and other novel atypical antipsychotics will instead of antagonizing D₂ receptors, will act as partial agonists, as well as agonists towards 5-HT_1A receptors. ^[2]

An NDA for Bifeprunox was filed by the US FDA in January, 2007. The FDA rejected the application in August, 2007.^[3] In the EU, Bifeprunox is still in Phase III clinical trials.

References

^ Towards a New Generation of Potential Antipsychotic Agents Combining D₂ and 5-HT_1A Receptor Activities, Journal of Medicinal Chemistry, Cuisiat et al. 2006
^ Pharmacological profiles in rats of novel antipsychotics with combined dopamine D₂/serotonin 5-HT_1A activity: comparison with typical and atypical conventional antipsychotics. Behavioural Pharmacology, Bardin et al. 2007
^ Wyeth and Solvay say FDA rejects application for antipsychotic drug bifeprunox. Thomson Financial, August 10, 2007.