Centanafadine  (Synonyms: EB-1020)

Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC₅₀s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.

IC50: 6 nM (human NE), 38 nM (human DA), 83 nM (human serotonin)^[1].

Centanafadine (EB-1020) preferentially inhibits monoamine reuptake in cloned cell lines transfected with human transporters with IC₅₀ values of 6 and 38 nM, respectively, for NE and DA transporters, Centanafadine has lesser effects on 5-HT transporter as it inhibits the reuptake of 5-HT with an IC₅₀ value of 83 nM ^[1].

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

In microdialysis studies, Centanafadine markedly increases NE, and DA concentrations levels in rat prefrontal cortex in vivo with peak increases of 375 and 300%, respectively with the greatest effects on NE, and also increases DA extracellular concentrations in the striatum to 400% of baseline concentrations. Behavioral studies demonstrate that Centanafadine dose-dependently decreases immobility in the mouse tail suspension test of depression to 13% of control levels, and do not stimulate locomotor activity in adult rats in the optimal dose range. Centanafadine dose-dependently inhibits locomotor hyperactivity in juvenile rats lesioned with the neurotoxin 6-hydroxydopamine (100 μg intracisternally) as neonates; a well-established animal model for attention-deficit hyperactivity disorder (ADHD)^[1].

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

209.29

C₁₅H₁₅N

924012-43-1

Solid

White to off-white

[C@@H]12[C@@](CNC2)(C3=CC(C=CC=C4)=C4C=C3)C1

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Bymaster FP, et al. Pharmacological characterization of the norepinephrine and dopamine reuptake inhibitor EB-1020: implications for treatment of attention-deficit hyperactivity disorder. Synapse. 2012 Jun;66(6):522-32.  [Content Brief]