| CAS NO: | 101152-94-7 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 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) | |
| Other info | Chemical Name:
(1R,2S)-2-(aminomethyl)-N,N-diethyl-1-phenylcyclopropane-1-carboxamide hydrochloride InChi Key: XNCDYJFPRPDERF-PBCQUBLHSA-N InChi Code: InChI=1S/C15H22N2O.ClH/c1-3-17(4-2)14(18)15(10-13(15)11-16)12-8-6-5-7-9-12;/h5-9,13H,3-4,10-11,16H2,1-2H3;1H/t13-,15+;/m1./s1 SMILES Code: O=C([C@@]1(C2=CC=CC=C2)[C@@H](CN)C1)N(CC)CC |
| Synonyms | Levomilnacipran, F-2207, Ixel, Savella, Dalcipran, Toledomin |
| 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. |
|---|---|
| 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. |
| Animal model | Rats |
| Formulation & Dosage | 10 and 30 mg/kg, PO |
| 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. |
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