924012-43-1
924012-43-1 structure
- Name: Centanafadine Hydrochloride
- Chemical Name: Centanafadine
- CAS Number: 924012-43-1
- Molecular Formula: C15H15N
- Molecular Weight: 209.286
- Catalog: Signaling Pathways GPCR/G Protein Adrenergic Receptor
- Create Date: 2018-10-17 20:17:46
- Modify Date: 2024-01-08 18:32:53
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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.
| Name | Centanafadine |
|---|---|
| Synonyms |
3-Azabicyclo[3.1.0]hexane, 1-(2-naphthalenyl)-, (1R,5S)-
EB-1020 D2A6T4UH9C (1R,5S)-1-(naphthalen-2-yl)-3-azabicyclo[3.1.0]hexane UNII-D2A6T4UH9C (1R,5S)-1-(2-Naphthyl)-3-azabicyclo[3.1.0]hexane DOV 216,419 Centanafadine Centanafadine Hydrochloride |
| 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. |
|---|---|
| Related Catalog | |
| 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 |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 363.5±11.0 °C at 760 mmHg |
| Molecular Formula | C15H15N |
| Molecular Weight | 209.286 |
| Flash Point | 187.3±14.7 °C |
| Exact Mass | 209.120453 |
| LogP | 2.74 |
| Vapour Pressure | 0.0±0.8 mmHg at 25°C |
| Index of Refraction | 1.679 |