Milnacipran HCl

Catalog No.S3140

Milnacipran HCl Chemical Structure

Molecular Weight(MW): 282.81

Milnacipran inhibits both norepinephrine transporter (NET) and norepinephrine transporter (SERT) with IC50 of 77 nM and 420 nM, respectively.

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 270 In stock
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Biological Activity

Description Milnacipran inhibits both norepinephrine transporter (NET) and norepinephrine transporter (SERT) with IC50 of 77 nM and 420 nM, respectively.
Targets
norepinephrine transporter (NET) [1] norepinephrine transporter (SERT) [1]
77 nM 420 nM
In vitro

Milnacipran is mainly excreted in the urine as the parent and glucoronide (> 80%), and only a small fraction (< 10%) is metabolized via N-de-ethylation by the CYP3A4 enzyme. [1] Milnacipran at high concentration can inhibit certain ligand-gated ion-channel (LGIC) receptors, including NMDA, 5-HT3A and nACh receptors, with IC50 of 58.4 μM, 185 μM, 14.3 μM. [2]

In vivo Milnacipran (10 and 30 mg/kg, PO) causes a dose-related increase in the extracellular levels of 5-HT and NA in the medial prefrontal cortex of rats. Milnacipran (30 and 60 mg/kg, PO) significantly reduces the duration of both the immobility time in the forced swimming test and the freezing time in the conditioned fear stress test in rats, which are animal behavioral models for depression and anxiety, respectively. [3] Milnacipran (<40 mg/kg i.p.) dose-dependently increases the extracellular levels of NA and 5-HT in hypothalamus of freely moving guinea pigs. Milnacipran administrated at 10 mg/kg and 40 mg/kg decreases NA metabolite MHPG levels by 57% and 47%, respectively, in hypothalamus of freely moving guinea pigs. [4]

Protocol

Solubility (25°C)

In vitro DMSO 57 mg/mL (201.54 mM)
Water 57 mg/mL (201.54 mM)
Ethanol 57 mg/mL (201.54 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 282.81
Formula

C15H22N2O.HCl

CAS No. 101152-94-7
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03569475 Recruiting Major Depressive Disorder Allergan July 6 2018 Phase 3
NCT03569475 Recruiting Major Depressive Disorder Allergan July 6 2018 Phase 3
NCT03249311 Recruiting None (i.e. Healthy Volunteers) University of Ottawa|Allergan March 2 2018 Phase 4
NCT03249311 Recruiting None (i.e. Healthy Volunteers) University of Ottawa|Allergan March 2 2018 Phase 4
NCT03128021 Recruiting Major Depressive Disorder Howard Aizenstein|Weill Cornell Institute of Geriatric Psychiatry|National Institute of Mental Health (NIMH)|University of Pittsburgh May 24 2017 Phase 4
NCT03128021 Recruiting Major Depressive Disorder Howard Aizenstein|Weill Cornell Institute of Geriatric Psychiatry|National Institute of Mental Health (NIMH)|University of Pittsburgh May 24 2017 Phase 4

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5-HT Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID