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
- 화학식: C19H23NO3
- 분자량:313.39
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Adrenergic Receptor Isoforms
More
Biological Activity
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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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분자량 313.39
-
화학식 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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선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)