Milnacipran hydrochloride

SKU: orb1309465

Description

Milnacipran hydrochloride is a serotonin-norepinephrine reuptake inhibitor (SNRI) used in depression research. It is the enantiomer of the fibromyalgia treatment milnacipran. This compound is applied in neuropharmacology studies, including in vitro transporter assays and in vivo behavioral models, and has been associated with rare, transient serum aminotransferase elevations.

Research Area

Cell Biology, Neuroscience

Key Properties

• CAS Number: 101152-94-7
• MW: 282.81
• Purity: 99.92%
• Formula: C₁₅H₂₃ClN₂O
• SMILES: Cl.C1[C@@H]([C@@]1(C(=O)N(CC)CC)c1ccccc1)CN
• Target: Norepinephrine,PERK,Serotonin Transporter
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (7.07 mM);H2O:28.3 mg/mL (100.07 mM);DMSO:50 mg/mL (176.8 mM)

Bioactivity

• Target IC50:
  SERT:420 nM|NET:77 nM
• In Vivo:
  Over 80% of Milnacipran is excreted in the urine primarily in its unchanged form and as glucuronide conjugates, with less than 10% metabolized through CYP3A4 enzyme-mediated N-deethylation. At high concentrations, Milnacipran can inhibit certain ligand-gated ion channel receptors, including 5-HT3A (IC50: 185 μM), NMDA (IC50: 58.4 μM), and nACh (IC50: 14.3 μM) receptors.
• In Vitro:
  In rat prefrontal cortex, Milnacipran (10 and 30 mg/kg, p.o.) was found to dose-dependently increase extracellular levels of NA and 5-HT. In antidepressant animal behavioral models, Milnacipran (30 and 60 mg/kg, p.o.) significantly reduced immobility time in the forced swim test in rats. Similarly, in animal models of anxiety, Milnacipran (30 and 60 mg/kg, p.o.) notably decreased immobility time in the conditioned fear stress test. In freely moving guinea pigs' hypothalamus, treatment with Milnacipran (10 mg/kg and 40 mg/kg) resulted in a 57% and 47% reduction in the NA metabolite MHPG respectively. Furthermore, Milnacipran (<40 mg/kg, i.p.) increased extracellular levels of NA and 5-HT in the hypothalamus of freely moving guinea pigs in a dose-dependent manner.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Serotonin Transporter, SerotoninTransporter, SERT, SLC6A4, Savella, 5-HTT, Dalcipran, Inhibitor, inhibit, norepinephrine transporter (NET), norepinephrine transporter (SERT), Milnacipran HCl, Milnacipran hydrochloride, Milnacipran Hydrochloride, Milnacipran

Compound Identifiers

PubChem CID

163701