Liafensine  (Synonyms: BMS-820836)

Liafensine (BMS-820836) is an orally active, blood-brain barrier-permeable monoamine reuptake inhibitor, with an IC₅₀ of 5.67 nM against DAT, 1.08 nM against SERT, and 7.99 nM against NET. Liafensine binds to DAT to block dopamine reuptake. Liafensine binds to SERT to block serotonin reuptake. Liafensine binds to NET to block norepinephrine reuptake. Liafensine can be used in studies related to depression^[1][2].

IC₅₀: 1.08 nM (serotonin transporter), 5.67 nM (dopamine transporter), 7.99 nM (norepinephrine transporter)

Liafensine potently inhibits monoamine reuptake in embryonic kidney 293 cells expressing SERT, DAT and NET, with IC₅₀ values of 1.08 nM, 5.67 nM and 7.99 nM, respectively^[1].

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

Liafensine (0.3 mg/kg) produces a 77% reduction in immobility in the mouse tail suspension model of depression^[1].

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

366.46

C₂₄H₂₂N₄

1198790-53-2

Solid

Light yellow to brown

NC1=NN=C(C2=CC3=C(C=C2)[C@H](C4=CC=C5C=CC=CC5=C4)CN(C)C3)C=C1

Room temperature in continental US; may vary elsewhere.

• [1]. Risinger R, et al. Evaluation of safety and tolerability, pharmacokinetics, and pharmacodynamics of BMS-820836 in healthy subjects: a placebo-controlled, ascending single-dose study. Psychopharmacology (Berl). 2014 Jun;231(11):2299-310.  [Content Brief]

  [2]. Bhagwagar Z, et al. Assessment of the Efficacy and Safety of BMS-820836 in Patients With Treatment-Resistant Major Depression: Results From 2 Randomized, Double-Blind Studies. J Clin Psychopharmacol. 2015 Aug;35(4):454-9.