1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. 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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Esreboxetine

Esreboxetine Chemische Struktur

CAS. Nr. : 98819-76-2

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Beschreibung

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[1].

Cellular Effect
Cell Line Type Value Description References
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]
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]
Klinische Studie
Molekulargewicht

313.39

Formel

C19H23NO3

CAS. Nr.
SMILES

CCOC(C=CC=C1)=C1O[C@H]([C@]2([H])CNCCO2)C3=CC=CC=C3

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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Esreboxetine
Art. -Nr.:
HY-14790
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