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Centanafadine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Centanafadine图片
CAS NO:924012-43-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
EB-1020
产品介绍
Centanafadine 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。
生物活性

Centanafadine is dualnorepinephrine (NE)/dopamine (DA)transporter inhibitor, also inhibitsserotonin transporter, withIC50sof 6 nM, 38 nM and 83 nM for human NE, DA andserotonin transporter, respectively.

IC50& Target

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

体外研究
(In Vitro)

Centanafadine (EB-1020) preferentially inhibits monoamine reuptake in cloned cell lines transfected with human transporters with IC50values 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 IC50value of 83 nM[1].

体内研究
(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)[1].

Clinical Trial
分子量

209.29

Formula

C15H15N

CAS 号

924012-43-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.