Centanafadine hydrochloride产品参数：
CAS No.：923981-14-0
MCE 际站：Centanafadine hydrochloride
产品活性：Centanafadine (hydrochloride) 是去甲肾上腺素(NE)/多巴胺(DA)转运的双抑制剂，还能抑制5-羟色胺(serotonin)转运体，其对人 NE，DA 和5-羟色胺转运体的IC50值分别为6 nM，38 nM 和 83 nM。
研究领域：GPCR/G Protein|Neuronal Signaling
作用靶点：Adrenergic Receptor|Dopamine Transporter|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).
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