产品
编 号：F331860
分子式：C24H23N3O2
分子量：385.46
分子式：C24H23N3O2
分子量：385.46
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CAS No: 350992-10-8
产品详情
生物活性：
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.
体内研究：
Bifeprunox (0.001-2.5 mg/kg) reduces marble burying in mice.Bifeprunox (4-250 μg/kg) influences nicotine-seeking behaviour in response to drug-associated stimuli in rats.Animal Model:Male NMRI mice (weighing 20-22 g)
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:Na?ve male Wistar rats (weighing 250-275 g)
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.
体外研究：
Bifeprunox has a pKi of 8 at h5-HT1A receptors, with an Emax of 70%.
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.
体内研究：
Bifeprunox (0.001-2.5 mg/kg) reduces marble burying in mice.Bifeprunox (4-250 μg/kg) influences nicotine-seeking behaviour in response to drug-associated stimuli in rats.Animal Model:Male NMRI mice (weighing 20-22 g)
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:Na?ve male Wistar rats (weighing 250-275 g)
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.
体外研究：
Bifeprunox has a pKi of 8 at h5-HT1A receptors, with an Emax of 70%.
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