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-HT1A 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-HT1A 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.

References


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