A SERT, DAT, and NET inhibitor
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Bicifadine (hydrochloride)

Item No. 43813

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(4-methylphenyl)-3-azabicyclo[3.1.0]hexane, monohydrochloride
CAS Number
66504-75-4
Molecular Formula
C12H15N • HCl
Formula Weight
209.7
Purity
≥90%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
CC1=CC=C(C23CNCC2C3)C=C1.Cl
InChi Code
InChI=1S/C12H15N.ClH/c1-9-2-4-10(5-3-9)12-6-11(12)7-13-8-12;/h2-5,11,13H,6-8H2,1H3;1H
InChi Key
OTZOPAFTLUOBOM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $45

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    5 mg

    $214

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    10 mg

    $383

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    25 mg

    $844

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    Product Description

    Bicifadine is an inhibitor of the serotonin transporter (SERT), dopamine transporter (DAT), and norepinephrine transporter (NET).1 It binds these transporters (Kis = 2.4, 5.2, and 5.4 µM, respectively) and inhibits serotonin, dopamine, and norepinephrine reuptake in intact cells expressing the human transporters (IC50s = 117, 910, and 55 nM, respectively). Bicifadine increases the mechanical withdrawal threshold in a rat model of acute inflammatory pain induced by subplantar injection of brewer’s yeast (ED50 = 9.2 mg/kg) and decreases writhing in mouse model of persistent abdominal pain induced by phenyl-p-quinone (PPQ; ED50 = 13.2 mg/kg). It also reduces paw licking in the first and second phases of the formalin test in mice and rats when administered 30 minutes prior to formalin.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Basile, A.S., Janowsky, A., Golembiowska, K., et al. Characterization of the antinociceptive actions of bicifadine in models of acute, persistent, and chronic pain. J. Pharmacol. Exp. Ther. 321(3), 1208-1225 (2007).