2. Neuronal Signaling
  3. Serotonin Transporter Dopamine Transporter
  4. 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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D-473

D-473 Chemical Structure

CAS No. : 1632000-05-5

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D-473 Related Antibodies

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Description

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[1].

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 (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 Related Antibodies
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.
Molecular Weight

439.49

Formula

C26H27F2NO3
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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D-473 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

D-4731632000-05-5D473D 473Serotonin TransporterDopamine Transporter5-HTTSERTSLC6A4DATSLC6A3hNEThDAThSERTmajor depressive disorderdopamine transporterhuman histamine H2 receptorsHEK 293 cellsnorepinephrine transporterserotonin transporterratInhibitorinhibitorinhibit

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