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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 350992-10-8
- Fòrmula: C24H23N3O2
- Peso molecular:385.46
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Ver todos los productos específicos de isoformas Dopamine Receptor
MoreVer todos los productos específicos de isoformas 5-HT Receptor
More
Actividad biológica
|
5-HT1A Receptor 7.19 (pKi, cortex) |
5-HT1A Receptor |
D2 Receptor 8.83 (pKi, striatum) |
5-HT1A Receptor 6.37 (pEC50, hippocampus) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
2.9 nM
Compound: 1b
|
Antagonist activity at human D2 dopamine receptor expressed in CHO cell membrane by GTPgammaS-binding assay
Antagonist activity at human D2 dopamine receptor expressed in CHO cell membrane by GTPgammaS-binding assay
|
[PMID: 23237836] |
Bifeprunox has a pKi of 8 at h5-HT1A receptors, with an Emax of 70%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Bifeprunox (4-250 μg/kg) influences nicotine-seeking behaviour in response to drug-associated stimuli in rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 350992-10-8
-
Peso molecular 385.46
-
Fòrmula C24H23N3O2
-
SMILES
O=C1OC2=C(N3CCN(CC4=CC=CC(C5=CC=CC=C5)=C4)CC3)C=CC=C2N1
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Bifeprunox Related Classifications
HY-14547 Related Classifications
Powered by Bioz