Levomilnacipran
Based on 1 publication(s) in Google Scholar
Levomilnacipran ((1S,2R)-Milnacipran) is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran is a serotonin and norepinephrine reuptake inhibitor, with IC50 values of 10.5 nM and 19.0 nM, and Ki values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression.
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- CAS No.: 96847-54-0
- 화학식: C15H22N2O
- 분자량:246.35
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보관:
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
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Levomilnacipran
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
320 nM
Compound: R-1, 1S,2R-milnacipran
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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: 18468895] |
| HEK293 | IC50 |
3200 nM
Compound: R-1, 1S,2R-milnacipran
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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: 18468895] |
| HEK293 | IC50 |
40 nM
Compound: R-1, 1S,2R-milnacipran
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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: 18468895] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Wistar rats aged 9 weeks old (200-220 g) treated LPS (HY-D1056)[3]
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Dosage:30 mg/kg
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Administration:Intraperitoneal injection; 10 days
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Result:Significantly ameliorated depression-like behaviors, including increasing sucrose preference in the SPT, reducing immobility time and increasing swimming time in the FST, and increasing the time spent in the central area in the OFT.
Improved neuronal synaptic deficits and morphological changes in the hippocampus, upregulated the expression of synaptic-related proteins PSD-95 and Syn, activated the BDNF/TrkB mediated PI3K/Akt/mTOR signaling pathway, and suppressed neuroinflammation by regulating the balance of pro- and anti-inflammatory cytokines in the hippocampus.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 96847-54-0
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분자량 246.35
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화학식 C15H22N2O
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SMILES
O=C(N(CC)CC)[C@@]1([C@@H](C1)CN)C2=CC=CC=C2
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Synonyms
(1S,2R)-Milnacipran; F2695
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell
2025 Nov 26;188(24):6861-6872.e14. PMID: 41138730
순도&문서
References
[1]. Asnis GM, et al. Levomilnacipran for the treatment of major depressive disorder: a review. Neuropsychiatr Dis Treat. 2015 Jan 9;11:125-35. [Content Brief]
[2]. Bundgaard C, et al. P-glycoprotein differentially affects escitalopram, levomilnacipran, vilazodone and vortioxetine transport at the mouse blood-brain barrier in vivo. Neuropharmacology. 2016 Apr;103:104-11. [Content Brief]
[3]. Wu Y, et al. Levomilnacipran Improves Lipopolysaccharide-Induced Dysregulation of Synaptic Plasticity and Depression-Like Behaviors via Activating BDNF/TrkB Mediated PI3K/Akt/mTOR Signaling Pathway. Mol Neurobiol. 2024 Jul;61(7):4102-4115. [Content Brief]
[4]. Auclair AL, et al. Levomilnacipran (F2695), a norepinephrine-preferring SNRI: profile in vitro and in models of depression and anxiety. Neuropharmacology. 2013 Jul;70:338-47. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Levomilnacipran Related Classifications
HY-14794A Related Classifications
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