您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Centanafadine(EB-1020)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Centanafadine(EB-1020)
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(EB-1020)图片
规格:98%
分子量:209.29
包装与价格:
包装价格(元)
250mg电议
500mg电议

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6nM,38nM和83nM。
货号:ajcx12560
CAS:924012-43-1
分子式:C15H15N
分子量:209.29
溶解度:Soluble in DMSO
纯度:98%
存储:Store at -20°C
库存:现货

Background:

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.

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].

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].

[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.