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 No.: 1632000-05-5
- Formule: C26H27F2NO3
- Masse moléculaire:439.49
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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 (Ki=9.18 nM), followed by hNET (Ki=39.7 nM) and hDAT (Ki=70.4 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
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Animal Model:Sprague-Dawley rat with major depressive disorder (male, 200-225 g)[1]
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Dosage:5 mg/kg; 10 mg/kg; 25 mg/kg; 50 mg/kg
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Administration:p.o.; single dose; 1 hour prior to 5-minute swim test
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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
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CAS No. 1632000-05-5
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Masse moléculaire 439.49
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Formule C26H27F2NO3
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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