Bifeprunox mesylate 

Bifeprunox mesylate is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pK_is 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 mesylate is an antipsychotic for the research of schizophrenia^[1][2].

Bifeprunox has a pK_i of 8 at h5-HT1A receptors, with an E_max of 70%^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

481.56

C₂₅H₂₇N₃O₅S

350992-13-1

Solid

Light yellow to light brown

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

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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]