product name Milnacipran HCl
Description: Milnacipran inhibits both norepinephrine transporter (NET) and norepinephrine transporter (SERT) with IC50 of 77 nM and 420 nM, respectively. 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. 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.
References: Bioorg Med Chem Lett. 2008 Feb 15;18(4):1346-9; Psychopharmacology (Berl). 2004 Sep;175(2):241-6; Psychopharmacology (Berl). 2002 Jul;162(3):323-32.
282.81
Formula
C15H22N2O.HCl
CAS No.
101152-94-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 57 mg/mL (201.5 mM)
Water: 57 mg/mL (201.5 mM)
Ethanol: 57 mg/mL (201.5 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. 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. |
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| Formulation & Dosage | |
| References | Bioorg Med Chem Lett. 2008 Feb 15;18(4):1346-9; Psychopharmacology (Berl). 2004 Sep;175(2):241-6; Psychopharmacology (Berl). 2002 Jul;162(3):323-32. |
