Centanafadine hydrochloride 是一种去甲肾上腺素(NE)/多巴胺(DA)转运的双抑制剂，还能抑制5-羟色胺(serotonin)转运体。它对人 NE，DA 和5-羟色胺转运体的IC50值分别为6 nM，38 nM 和 83 nM。

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).

Centanafadine (EB-1020) preferentially inhibits monoamine reuptake in cloned cell lines transfected with human transporters (IC50s: 6 and 38 nM), for NE and DA transporters, Centanafadine has lesser effects on 5-HT transporter as it inhibits the reuptake of 5-HT (IC50: 83 nM).

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. 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 intracisternal) as neonates.

923981-14-0

C15H16ClN

245.75

EB-1020 hydrochloride

DMSO:125 mg/mL (508.65 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years