Centanafadine hydrochloride

Centanafadine hydrochloride is a dual inhibitor of norepinephrine (NE) /dopamine (DA) transporter, also inhibits serotonin transporter (IC50s: 6 nM, 38 nM, and 83 nM for human NE, DA, and serotonin transporter) . (In Vitro) :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 . (In Vivo) :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) .

923981-14-0

EB-1020 hydrochloride

>98% (HPLC)

DMSO:125 mg/mL (508.65 mM; Need ultrasonic)

[H][C@@]12CNC[C@]1 (C3=CC=C4C=CC=CC4=C3) C2.[H]Cl

C15H16ClN

245.75

Storage temperature: -20°C. Stability: ≥ 2 years