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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].

Product Specifications

CAS Number

[350992-10-8]

UNSPSC

12352005

Target

5-HT Receptor; Dopamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/bifeprunox.html

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C24H23N3O2

Molecular Weight

385.46

References & Citations

[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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

5-HT1 Receptor; D2 Receptor; mLAG-3

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