Bifeprunox

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IUPAC_name = 7- [4- [(3-Phenylphenyl)methyl] piperazin-1-yl] -"3H"-benzooxazol-2-one

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PubChem = 208951
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C=24|H=23|N=3|O=2
molecular_weight = 385.458 g/mol
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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. [cite journal |author=Cuisiat S, Bourdiol N, Lacharme V, Newman-Tancredi A, Colpaert F, Vacher B |title=Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities |journal=J. Med. Chem. |volume=50 |issue=4 |pages=865–76 |year=2007 |pmid=17300168 |doi=10.1021/jm061180b]

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. [cite journal |author=Bardin L, Auclair A, Kleven MS, "et al" |title=Pharmacological profiles in rats of novel antipsychotics with combined dopamine D2/serotonin 5-HT1A activity: comparison with typical and atypical conventional antipsychotics |journal=Behav Pharmacol |volume=18 |issue=2 |pages=103–18 |year=2007 |pmid=17351418 |doi=10.1097/FBP.0b013e3280ae6c96]

An NDA for Bifeprunox was filed by the US FDA in January, 2007. The FDA rejected the application in August, 2007. [ [http://www.finanznachrichten.de/nachrichten-2007-08/artikel-8796651.asp Wyeth and Solvay say FDA rejects application for antipsychotic drug bifeprunox.] Thomson Financial, August 10, 2007.] In the EU, Bifeprunox is still in Phase III clinical trials.

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