Name | 7-[4-[(3-phenylphenyl)methyl]piperazin-1-yl]-3H-1,3-benzoxazol-2-one |
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Synonyms |
Bifeprunox [INN]
UNII-AP69E83Z79 Bifeprunoxum Bifeprunox (USAN/INN) bifeprunox base Bifeprunoxum [INN-Latin] 2-[4-[4-(5-fluoro-1H-indol-3-yl)-3,6-dihydro-1(2H)-pyridinyl]butyl]-1H-isoindole-1,3(2H)-dione Bifeprunox 7-[4-[(3-phenylphenyl)methyl]piperazin-1-yl]-3H-benzooxazol-2-one 7-[4-([1,1'-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxa-zolone |
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]. |
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Related Catalog | |
Target |
5-HT1A Receptor:7.19 (pKi, cortex) D2 Receptor:8.83 (pKi, striatum) 5-HT1A Receptor:6.37 (pEC50, hippocampus) |
In Vitro | Bifeprunox has a pKi of 8 at h5-HT1A receptors, with an Emax of 70%[1]. |
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. |
References |
Density | 1.247g/cm3 |
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Molecular Formula | C24H23N3O2 |
Molecular Weight | 385.45800 |
Exact Mass | 385.17900 |
PSA | 52.48000 |
LogP | 4.11320 |
Index of Refraction | 1.643 |
HS Code | 2934999090 |
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HS Code | 2934999090 |
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Summary | 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |