Centanafadine hydrochloride

SKU: orb1309848

Description

Centanafadine hydrochloride

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 923981-14-0
• MW: 245.75
• Purity: 99.66%
• Formula: C₁₅H₁₆ClN
• SMILES: Cl.C1[C@@H]2CNC[C@]12c1ccc2ccccc2c1
• Target: Dopamine Receptor,Norepinephrine,Adrenergic Receptor,Serotonin Transporter
• Solubility: DMSO:125 mg/mL (508.65 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (16.28 mM)

Bioactivity

• Target IC50:
  Dopamine:38 nM (human)|Norepinephrine:6 nM (human)|5-HT:83 nM(human)
• In Vivo:
  In microdialysis studies, Centanafadine significantly increases NE and DA concentrations in the rat prefrontal cortex in vivo, with peak increases of 375% and 300%, respectively, showing the greatest effects on NE. It also raises DA extracellular concentrations in the striatum to 400% of baseline levels. Centanafadine dose-dependently reduces immobility in the mouse tail suspension test of depression to 13% of control levels without stimulating locomotor activity in adult rats at the optimal dose range. Additionally, it dose-dependently inhibits locomotor hyperactivity in juvenile rats lesioned with the neurotoxin 6-hydroxydopamine (100 μg intracisternal) as neonates.
• In Vitro:
  Centanafadine (EB-1020) preferentially inhibits monoamine reuptake in cloned cell lines transfected with human transporters, with IC50 values of 6 nM for NE and 38 nM for DA transporters. It has a lesser effect on the 5-HT transporter, inhibiting 5-HT reuptake with an IC50 of 83 nM.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Centanafadine, Centanafadine hydrochloride, Centanafadine Hydrochloride, Beta Receptor, DAT, DopamineReceptor, Dopamine Receptor, Dopamine Transporter, dopamine, 5-HTT, Adrenergic Receptor, AdrenergicReceptor, Inhibitor, human NE, human serotonin, human DA, EB 1020, EB 1020 Hydrochloride, EB-1020, EB1020 Hydrochloride, EB-1020 hydrochloride, EB-1020 Hydrochloride, EB1020, inhibit, Norepinephrine (NE), SERT, Serotonin Transporter, SerotoninTransporter, serotonin, SLC6A4, SLC6A3

Compound Identifiers

PubChem CID

68943792