CAS 350992-10-8|Bifeprunox
Introduction：Basic information about CAS 350992-10-8|Bifeprunox, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Bifeprunox | ||
|---|---|---|---|
| CAS Number | 350992-10-8 | Molecular Weight | 385.45800 |
| Density | 1.247g/cm3 | Boiling Point | / |
| Molecular Formula | C24H23N3O2 | Melting Point | / |
| MSDS | / | Flash Point | / |
Names
| Name | 7-[4-[(3-phenylphenyl)methyl]piperazin-1-yl]-3H-1,3-benzoxazol-2-one |
|---|---|
| Synonym | More Synonyms |
Bifeprunox BiologicalActivity
| 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 | Signaling Pathways >>GPCR/G Protein >>Dopamine ReceptorSignaling Pathways >>Neuronal Signaling >>Dopamine ReceptorResearch Areas >>Neurological DiseaseSignaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT Receptor |
| 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 |
| InChIKey | CYGODHVAJQTCBG-UHFFFAOYSA-N |
| SMILES | O=c1[nH]c2cccc(N3CCN(Cc4cccc(-c5ccccc5)c4)CC3)c2o1 |
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 |
