1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
    5-HT Receptor
  3. Bifeprunox

Bifeprunox 

Cat. No.: HY-14547
Handling Instructions

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.

For research use only. We do not sell to patients.

Bifeprunox Chemical Structure

Bifeprunox Chemical Structure

CAS No. : 350992-10-8

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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].

IC50 & Target[2]

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.
Molecular Weight

385.46

Formula

C₂₄H₂₃N₃O₂

CAS No.

350992-10-8

SMILES

O=C1OC2=C(N3CCN(CC4=CC=CC(C5=CC=CC=C5)=C4)CC3)C=CC=C2N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

BifeprunoxDopamine Receptor5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptordopamineD25-HT1AcortexstriatumhippocampusantipsychoticschizophreniaInhibitorinhibitorinhibit

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Bifeprunox
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