Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Centanafadine is a dual inhibitor of norepinephrine (NE)/dopamine (DA) transporter, also inhibits serotonin transporter (IC50s: 6 nM, 38 nM, and 83 nM for human NE, DA, and serotonin transporter).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,520.00 | |
50 mg | 6-8 weeks | $ 1,980.00 | |
100 mg | 6-8 weeks | $ 2,500.00 |
Description | Centanafadine is a dual inhibitor of norepinephrine (NE)/dopamine (DA) transporter, also inhibits serotonin transporter (IC50s: 6 nM, 38 nM, and 83 nM for human NE, DA, and serotonin transporter). |
Targets&IC50 | NE (human):6 nM , 5-HT (human):83 nM , DA (human):38 nM |
In vitro | Centanafadine (EB-1020) preferentially inhibits monoamine reuptake in cloned cell lines transfected with human transporters (IC50s: 6 and 38 nM), for NE and DA transporters, Centanafadine has lesser effects on 5-HT transporter as it inhibits the reuptake of 5-HT (IC50: 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. 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 intracisternal) as neonates. |
Synonyms | EB-1020 |
Molecular Weight | 209.29 |
Formula | C15H15N |
CAS No. | 924012-43-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Centanafadine 924012-43-1 Others EB1020 EB 1020 EB-1020 inhibitor inhibit