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Centanafadine hydrochloride

CAS No. : 923981-14-0

MCE 国际站：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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