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Bifeprunox

  Cat. No.:  DC8729   Featured
Chemical Structure
350992-10-8
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More than 5000 active chemicals with high quality for research!
Field of application
Dopamine D2 and 5-HT1A partial agonist in development as a potential treatment for schizophrenia and other psychotic indications; Pharmacoloy profile makes it an atypical antipsychotic and a new approach for the treatment of schizophrenia.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 350992-10-8
SMILES: C1CN(CCN1CC2=CC=CC(=C2)C3=CC=CC=C3)C4=CC=CC5=C4OC(=O)N5
Formula: C24H23N3O2
M.Wt: 385.46
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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[1][2].
Target: 5-HT1A Receptor:7.19 (pKi, cortex) D2 Receptor:8.83 (pKi, striatum) 5-HT1A Receptor:6.37 (pEC50, hippocampus)
In Vivo: Bifeprunox (0.001-2.5 mg/kg) reduces marble burying in mice[2]. Bifeprunox (4-250 μg/kg) influences nicotine-seeking behaviour in response to drug-associated stimuli in rats[3]. Animal Model: Male NMRI mice (weighing 20-22 g)[2] Dosage: 0.001, 0.0025, 0.01, 0.04, 0.16, 0.63, and 2.5 mg/kg Administration: I.p. Result: Reduced marble burying. Potently active from 0.0025 mg/kg. Animal Model: Naïve male Wistar rats (weighing 250-275 g)[3] Dosage: 4, 16, 64 and 250 μg/kg Administration: Injected s.c. 30 minutes before testing 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.
In Vitro: Bifeprunox has a pKi of 8 at h5-HT1A receptors, with an Emax of 70%[1].
References: [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. [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. [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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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