中文名:米那普仑盐酸盐
英文名:Milnacipran HCl
英文别名:(1R,2S)-2-(aminomethyl)-N,N-diethyl-1-phenylcyclopropanecarboxamide hydrochloride
纯度:10mM in DMSO
货号:M407971
包装:1ml
Cas号:101152-94-7
存储温度:-80℃储存
产品介绍:
Information
Milnacipran HCl Milnacipran inhibits both norepinephrine transporter (NET) and norepinephrine transporter (SERT) with IC50 of 77 nM and 420 nM, respectively.
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. 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.
Cell Data
cell lines:
Concentrations:
Incubation Time:
Powder Purity:≥99%
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关键字: (1R,2S)-2-(aminomethyl)-N,N-diethyl-1-phenylcyclopropanecarboxamide hydrochloride
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