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D-473

D-473 is an orally active, blood-brain barrier penetrant and serotonin-preferring reuptake inhibitor. D-473 inhibits serotonin, dopamine and norepinephrine transporters, and significantly elevates the extracellular levels of these three neurotransmitters in rat brain regions. D-473 exhibits definite antidepressant-like activity without inducing motor activation. D-473 is widely used in studies related to major depressive disorder.

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CAS. Nr.: 1632000-05-5
Formel: C₂₆H₂₇F₂NO₃
Molecular Weight:439.49

Speicherung:

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

D-473 Chemical Structure

CAS. Nr.: 1632000-05-5

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

In Vitro

D-473 (at least five triplicate concentrations spaced evenly around the IC₅₀ value) potently inhibits monoamine uptake in HEK 293 cells expressing cloned human hDAT, hSERT, and hNET, with highest potency for hSERT (K_i=9.18 nM), followed by hNET (K_i=39.7 nM) and hDAT (K_i=70.4 nM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

D-473 (5-50 mg/kg; p.o.; single dose; 1 hour prior to 5-minute swim test) produces dose-dependent, statistically significant reductions in immobility time in the rat forced swim test^[1].
D-473 (25 mg/kg; p.o.; single dose) does not significantly alter locomotor activity in rats^[1].
D-473 (10 mg/kg; i.p.; single dose) significantly elevates extracellular dopamine, serotonin, and norepinephrine in the rat mPFC and DLS, while reducing levels of dopamine metabolites in these regions^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Sprague-Dawley rat with major depressive disorder (male, 200-225 g)^[1]
Dosage:

5 mg/kg; 10 mg/kg; 25 mg/kg; 50 mg/kg
Administration:

p.o.; single dose; 1 hour prior to 5-minute swim test
Result:

Produced no significant reduction in immobility time at 5 mg/kg.
Reduced immobility time significantly compared to vehicle at 10 mg/kg.
Reduced immobility time significantly compared to vehicle at 25 mg/kg.
Reduced immobility time significantly compared to vehicle at 50 mg/kg.

Chemical Information

CAS. Nr. 1632000-05-5
Molecular Weight 439.49
Formel C₂₆H₂₇F₂NO₃
SMILES

O[C@@H]([C@@H](CO1)NCC2=CC=C(C=C2)OC)C[C@H]1C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Dutta AK, et al. Pharmacological and behavioral characterization of D-473, an orally active triple reuptake inhibitor targeting dopamine, serotonin and norepinephrine transporters. PLoS One. 2014;9(11):e113420. Published 2014 Nov 26. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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