Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Centanafadine hydrochloride (EB-1020 hydrochloride) 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).
説明 | Centanafadine hydrochloride (EB-1020 hydrochloride) 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). |
ターゲット&IC50 | Dopamine:38 nM (human), Norepinephrine:6 nM (human), 5-HT:83 nM(human) |
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. |
別名 | EB-1020 hydrochloride |
分子量 | 245.75 |
分子式 | C15H16ClN |
CAS No. | 923981-14-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (508.65 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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Centanafadine hydrochloride 923981-14-0 GPCR/G Protein Neuroscience Dopamine Receptor Serotonin Transporter Adrenergic Receptor Norepinephrine EB-1020 hydrochloride Centanafadine SLC6A3 5-HTT EB-1020 Hydrochloride EB 1020 Dopamine Transporter SLC6A4 Beta Receptor Centanafadine Hydrochloride DAT EB-1020 inhibit SERT EB1020 EB 1020 Hydrochloride EB1020 Hydrochloride Inhibitor inhibitor