Bifeprunox

Modify Date: 2024-01-12 00:47:20

Bifeprunox Structure
Bifeprunox structure
Common Name Bifeprunox
CAS Number 350992-10-8 Molecular Weight 385.45800
Density 1.247g/cm3 Boiling Point N/A
Molecular Formula C24H23N3O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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[1][2].

 Names

Name 7-[4-[(3-phenylphenyl)methyl]piperazin-1-yl]-3H-1,3-benzoxazol-2-one
Synonym More Synonyms

 Bifeprunox Biological Activity

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].
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

[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.

 Chemical & Physical Properties

Density 1.247g/cm3
Molecular Formula C24H23N3O2
Molecular Weight 385.45800
Exact Mass 385.17900
PSA 52.48000
LogP 4.11320
Index of Refraction 1.643

 Safety Information

HS Code 2934999090

 Customs

HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 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
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