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Milnacipran HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Milnacipran HCl图片
CAS NO:101152-94-7
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)282.81
FormulaC15H22N2O.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

实验参考方法
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 VivoMilnacipran (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 modelRats
Formulation & Dosage10 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.