Home Neuronal Signaling Serotonin Transporter inhibitor Milnacipran HCl For research use only.

Milnacipran HCl

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

Milnacipran HCl Chemical Structure

Milnacipran HCl Chemical Structure

CAS: 101152-94-7

Purity & Quality Control

Batch: S314001 DMSO] 57 mg/mL] false] Water] 57 mg/mL] false] Ethanol] 57 mg/mL] false Purity: 99.99%
99.99

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

Chemical lnformation & Solubility

Molecular Weight 282.81 Formula

C15H22N2O.HCl
CAS No. 101152-94-7 SDF Download Milnacipran HCl SDF
Smiles CCN(CC)C(=O)C1(CC1CN)C2=CC=CC=C2.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 57 mg/mL ( (201.54 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 57 mg/mL

Ethanol : 57 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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