(R,R)-Reboxetine mesylate
(R,R)-Reboxetine mesylate is an antidepressant agent with great bioavailability. (R,R)-Reboxetine is the enantiomer of Reboxetine, which is a selective noradrenaline reuptake inhibitor. Reboxetine consists of (R,R) and (S,S) enantiomer, has low affinity for alpha-adrenergic and muscarinic receptors and low toxicity in animals.
For research use only. We do not sell to patients.
- CAS No.: 105017-39-8
- Formula: C20H27NO6S
- Molecular Weight:409.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Adrenergic Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[2]|
α adrenergic receptor |
Muscarinic Receptors |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.005 μM
Compound: Reboxetine
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Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells
Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells
|
[PMID: 34112854] |
| HEK293 | IC50 |
0.005 μM
Compound: Reboxetine
|
Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 174586
Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 174586
|
[PMID: 34112854] |
Chemical Information
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CAS No. 105017-39-8
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Molecular Weight 409.50
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Formula C20H27NO6S
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SMILES
CCOC1=CC=CC=C1O[C@@H]([C@@]2([H])CNCCO2)C3=CC=CC=C3.CS(=O)(O)=O
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Synonyms
(R,R)-FCE20124 mesylate; (R,R)-PNU155950E mesylate; (R,R)-(-)-Reboxetine mesylate
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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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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
Purity & Documentation
References
[1]. Wienkers LC, et al. Cytochrome P-450-mediated metabolism of the individual enantiomers of the antidepressant agent reboxetine in human liver microsomes. Drug Metab Dispos. 1999 Nov;27(11):1334-40. [Content Brief]
[2]. Dostert P, et al. Review of the pharmacokinetics and metabolism of reboxetine, a selective noradrenaline reuptake inhibitor. Eur Neuropsychopharmacol. 1997 Apr;7 Suppl 1:S23-35; discussion S71-3. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)