Esreboxetine
Esreboxetine ((S,S)-Reboxetine) is a selective norepinephrine reuptake inhibitor with activity in increasing urethral resistance. Esreboxetine has been reported to be effective in patients with stress urinary incontinence in a Phase IIa clinical study, achieving this effect by increasing urethral closure. The mechanism of action of esreboxetine involves inhibition of norepinephrine transporters in the central and peripheral nervous systems. The peripheral selectivity of esreboxetine helps it significantly increase urethral resistance without penetrating the brain.
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- CAS No.: 98819-76-2
- Formule: C19H23NO3
- Masse moléculaire:313.39
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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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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10000 nM
Compound: 20
|
Inhibition of serotonin uptake at human SERT expressed in HEK293 cells
Inhibition of serotonin uptake at human SERT expressed in HEK293 cells
|
[PMID: 18672364] |
| HEK293 | IC50 |
3 nM
Compound: 20
|
Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells
Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells
|
[PMID: 18672364] |
| HEK293 | IC50 |
>10000 nM
Compound: 20
|
Inhibition of dopamine uptake at human DAT expressed in HEK293 cells
Inhibition of dopamine uptake at human DAT expressed in HEK293 cells
|
[PMID: 18672364] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 98819-76-2
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Masse moléculaire 313.39
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Formule C19H23NO3
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SMILES
CCOC(C=CC=C1)=C1O[C@H]([C@]2([H])CNCCO2)C3=CC=CC=C3
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Synonyms
(S,S)-(+)-Reboxetine
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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)