1. GPCR/G Protein
    Neuronal Signaling
  2. Adrenergic Receptor
    Dopamine Transporter
    Serotonin Transporter

Centanafadine (Synonyms: EB-1020)

Cat. No.: HY-16736
Handling Instructions

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.

For research use only. We do not sell to patients.

Centanafadine Chemical Structure

Centanafadine Chemical Structure

CAS No. : 924012-43-1

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Other Forms of Centanafadine:

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

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.

IC50 & 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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.7781 mL 23.8903 mL 47.7806 mL
5 mM 0.9556 mL 4.7781 mL 9.5561 mL
10 mM 0.4778 mL 2.3890 mL 4.7781 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

209.29

Formula

C₁₅H₁₅N

CAS No.

924012-43-1

SMILES

[[email protected]@H]12[[email protected]@](CNC2)(C3=CC(C=CC=C4)=C4C=C3)C1

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Centanafadine
Cat. No.:
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Centanafadine

Cat. No.: HY-16736