Bifeprunox
Bifeprunox is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC50 of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox is an antipsychotic for the research of schizophrenia.
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- CAS No.: 350992-10-8
- Formule: C24H23N3O2
- Masse moléculaire:385.46
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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5-HT1A Receptor 7.19 (pKi, cortex) |
5-HT1A Receptor |
D2 Receptor 8.83 (pKi, striatum) |
5-HT1A Receptor 6.37 (pEC50, hippocampus) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
2.9 nM
Compound: 1b
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Antagonist activity at human D2 dopamine receptor expressed in CHO cell membrane by GTPgammaS-binding assay
Antagonist activity at human D2 dopamine receptor expressed in CHO cell membrane by GTPgammaS-binding assay
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[PMID: 23237836] |
Bifeprunox has a pKi of 8 at h5-HT1A receptors, with an Emax of 70%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Bifeprunox (4-250 μg/kg) influences nicotine-seeking behaviour in response to drug-associated stimuli in rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male NMRI mice (weighing 20-22 g)[2]
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Dosage:0.001, 0.0025, 0.01, 0.04, 0.16, 0.63, and 2.5 mg/kg
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Administration:I.p.
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Result:Reduced marble burying. Potently active from 0.0025 mg/kg.
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Animal Model:Naïve male Wistar rats (weighing 250-275 g)[3]
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Dosage:4, 16, 64 and 250 μg/kg
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Administration:Injected s.c. 30 minutes before testing
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Result:4-16 μg/kg dose-dependently attenuated the responsereinstating effects of nicotine-associated cues. Higher doses (64-250 μg/kg, s.c.) reduced spontaneous locomotor activity and suppressed operant responding induced by sucrose-associated cues and by the primary reinforcing properties of nicotine or sucrose.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 350992-10-8
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Masse moléculaire 385.46
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Formule C24H23N3O2
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SMILES
O=C1OC2=C(N3CCN(CC4=CC=CC(C5=CC=CC=C5)=C4)CC3)C=CC=C2N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Newman-Tancredi A, et al. Novel antipsychotics activate recombinant human and native rat serotonin 5-HT1A receptors: affinity, efficacy and potential implications for treatment of schizophrenia. Int J Neuropsychopharmacol. 2005 Sep;8(3):341-56. [Content Brief]
[2]. Bruins Slot LA, et al. Effects of antipsychotics and reference monoaminergic ligands on marble burying behavior in mice. Behav Pharmacol. 2008 Mar;19(2):145-52. [Content Brief]
[3]. Di Clemente A, et al. Bifeprunox: a partial agonist at dopamine D2 and serotonin 1A receptors, influences nicotine-seeking behaviour in response to drug-associated stimuli in rats. Addict Biol. 2012 Mar;17(2):274-86. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Bifeprunox Related Classifications
HY-14547 Related Classifications
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