Esreboxetine
Esreboxetine ((S,S)-Reboxetine) is a selective norepinephrine transporter (NET) inhibitor, with a pIC50 of 9.6 and a pKi of 9.2 in rats, and it can cross the blood-brain barrier. Esreboxetine increases urethral closure pressure and urethral resistance in rats. Esreboxetine is applicable to research related to inflammatory pain and stress urinary incontinence.
For research use only. We do not sell to patients.
- CAS No.: 98819-76-2
- Formula: C19H23NO3
- Molecular Weight:313.39
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10000 nM
Compound: 20
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Inhibition of serotonin uptake at human SERT expressed in HEK293 cells
Inhibition of serotonin uptake at human SERT expressed in HEK293 cells
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[PMID: 18672364] |
| HEK293 | IC50 |
3 nM
Compound: 20
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Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells
Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells
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[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
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[PMID: 18672364] |
In Vitro
Esreboxetine (10 pM-100 μM; 6 h) exhibits 20,000-fold higher selectivity for the rat norepinephrine transporter over the serotonin transporter in in vitro radioligand binding assays, with a pKi of 9.2 for rat NET and 5.6 for rat SERT[1].
Esreboxetine (10 pM-100 μM; 30 min pre-incubation, 6 min incubation) potently and selectively inhibits norepinephrine uptake in rat cortical synaptosomes, with a pIC50 of 9.6 for rat NET and a pIC50 of 5.3 for rat SERT, representing a 20,000-fold selectivity for NET over SERT[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (adult male, 150-220 g, formalin-induced inflammatory pain model)[1]
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Dosage:10 mg/kg (esreboxetine); 1 mg/kg (Fluoxetine)
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Administration:i.p.; single dose
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Result:Produced 24% inhibition of flinching behavior in the rat formalin model.
Achieved 78% NET and 55% SERT ex vivo transporter occupancy at 75 minutes post-dose.
Shifted the morphine dose-response curve leftward, reducing the morphine ED50 to 0.3 mg/kg, consistent with potentiation of morphine's antinociceptive effect.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 98819-76-2
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Molecular Weight 313.39
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Formalin-Induced Paw Inflammation/Nociceptive Inflammation
The formalin-induced paw inflammation/nociceptive test is a chemical persistent pain model in rodents in which subcutaneous injection of formalin into the hind paw produces spontaneous nocifensive behaviors such as flinching and licking. The response is classically biphasic, consisting of an early acute phase (Phase I) reflecting direct activation of peripheral nociceptors (particularly C-fiber afferents), followed by a later prolonged phase (Phase II) associated with central sensitization in the spinal dorsal horn driven by sustained afferent input and inflammatory signaling. This model is widely used to evaluate analgesic and anti-inflammatory interventions because it captures both peripheral nociception and central sensitization processes within a single assay system.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Esreboxetine Related Classifications
HY-14790 Related Classifications
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