Centanafadine hydrochloride

Modify Date: 2024-01-11 18:55:04

Centanafadine hydrochloride Structure
Centanafadine hydrochloride structure
Common Name Centanafadine hydrochloride
CAS Number 923981-14-0 Molecular Weight 245.747
Density N/A Boiling Point N/A
Molecular Formula C15H16ClN Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Centanafadine hydrochloride


Centanafadine (hydrochloride) 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.

 Names

Name Centanafadine hydrochloride
Synonym More Synonyms

 Centanafadine hydrochloride Biological Activity

Description Centanafadine (hydrochloride) 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.
Related Catalog
Target

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

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 [1].
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].
References

[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.

 Chemical & Physical Properties

Molecular Formula C15H16ClN
Molecular Weight 245.747
Exact Mass 245.097122

 Synonyms

(1R,5S)-1-(2-Naphthyl)-3-azabicyclo[3.1.0]hexanhydrochlorid (1:1)
EB-1020
3-Azabicyclo[3.1.0]hexane, 1-(2-naphthalenyl)-, (1R,5S)-, hydrochloride (1:1)
(1R,5S)-1-(2-Naphtyl)-3-azabicyclo[3.1.0]hexane, chlorhydrate (1:1)
UNII:265DN9X85W
(1R,5S)-1-(2-Naphthyl)-3-azabicyclo[3.1.0]hexane hydrochloride (1:1)
(1R,5S)-1-(naphthalen-2-yl)-3-azabicyclo[3.1.0]hexane hydrochloride
DOV 216,419
Centanafadine hydrochloride