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Centanafadine hydrochloride

Names

[ CAS No. ]:
923981-14-0

[ Name ]:
Centanafadine hydrochloride

[Synonym ]:
(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

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]:

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor
Signaling Pathways >> Neuronal Signaling >> Dopamine Transporter
Signaling Pathways >> Neuronal Signaling >> Serotonin Transporter
Research Areas >> Neurological Disease

[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.


[Related Small Molecules]

Isoprenaline hydrochloride | ICI 118,551 (hydrochloride) | Fluoxetine Hydrochloride | Phenylephrine hydrochloride | Yohimbine hydrochloride | Adrenaline | Ivabradine hydrochloride | Paroxetine HCl | Prazosin hydrochloride | Vanoxerine dihydrochloride | Clenbuterol hydrochloride | Sertraline hydrochloride | Phentolamine mesilate | Fluvoxamine maleat | guanfacine hydrochloride

Chemical & Physical Properties

[ Molecular Formula ]:
C15H16ClN

[ Molecular Weight ]:
245.747

[ Exact Mass ]:
245.097122

Related Compounds