Milnacipran HCl

For research use only.

Catalog No.S3140

Milnacipran HCl Chemical Structure

CAS No. 101152-94-7

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

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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.
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]


Solubility (25°C)

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

* 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


CAS No. 101152-94-7
Storage powder
in solvent
Synonyms N/A
Smiles CCN(CC)C(=O)C1(CC1CN)C2=CC=CC=C2.Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01329406 Unknown status Drug: Milnacipran|Drug: Placebo Osteoarthritis Analgesic Solutions|Forest Laboratories July 2011 Phase 4
NCT01328002 Terminated Drug: Milnacipran|Drug: Placebo Primary Fibromyalgia Forest Laboratories|Cypress Bioscience Inc. April 30 2011 Phase 2
NCT01418651 Terminated Drug: Savella Fibromyalgia Banner Health|Forest Laboratories March 2011 Phase 3
NCT01288807 Completed Drug: Milnacipram Fibromyalgia University of California San Diego|Forest Laboratories|US Department of Veterans Affairs February 2011 Phase 4
NCT00725101 Completed Drug: Treatment for Fibromyalgia Fibromyalgia Eli Lilly and Company June 2008 --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID