去甲氟西汀

去甲氟西汀用途

盐酸去甲氟西汀是氟西汀的一种活性N-去甲基代谢产物。氟西汀是一种选择性5-羟色胺(5-HT)再摄取抑制剂,通过细胞色素P450(CYP)2D6、CYP2C19和CYP3A4代谢为去甲氟西汀盐酸盐。去甲氟西汀盐酸盐抑制5-HT摄取并抑制CaV3.3 T电流(IC50=5μM)。盐酸去甲氟西汀具有抗惊厥活性[1][2][3][4]。

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去甲氟西汀名称

[ CAS 号 ]:
57226-68-3

[ 中文名 ]:
去甲氟西汀

[ 英文名 ]:
Norfluoxetine hydrochloride

[英文别名 ]:

去甲氟西汀生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

[ 靶点 ]

5-HT Receptor

Cav3.3:5 μM (IC50)

[体内研究]

用氟西汀或盐酸去甲氟西汀(20mg/kg皮下注射)以及苯妥英钠(30mg/kg腹腔注射)和氯硝西泮(0.1mg/kg静脉注射)预处理可显著提高存活率和持续时间,对戊四氮诱发的癫痫具有显著的保护作用[1]。

[参考文献]

[1]. Valéria Kecskeméti, et al. Norfluoxetine and fluoxetine have similar anticonvulsant and Ca2+ channel blocking potencies. Brain Res Bull. 2005 Sep 30;67(1-2):126-32.

[2]. Achraf Traboulsie, et al. T-type calcium channels are inhibited by fluoxetine and its metabolite norfluoxetine. Mol Pharmacol. 2006 Jun;69(6):1963-8.

[3]. Hyeon-Cheol Jeong, et al. Prediction of Fluoxetine and Norfluoxetine Pharmacokinetic Profiles Using Physiologically Based Pharmacokinetic Modeling. Clin Pharmacol. 2021 Nov;61(11):1505-1513.

[4]. D T Wong, et al. Norfluoxetine enantiomers as inhibitors of serotonin uptake in rat brain. Neuropsychopharmacology. 1993 Jun;8(4):337-44.

去甲氟西汀物理化学性质

[ 密度 ]:
1.204g/cm3

[ 沸点 ]:
381.1ºC at 760 mmHg

[ 分子式 ]:
C₁₆H₁₇ClF₃NO

[ 分子量 ]:
331.760

[ 闪点 ]:
184.3ºC

[ 精确质量 ]:
331.095062

[ PSA ]:
35.25000

[ LogP ]:
5.67660

[ 外观性状 ]:
黄色固体

[ 储存条件 ]:
-20°C，密闭，干燥

[ 水溶解性 ]:
H2O: >4 mg/mL

去甲氟西汀MSDS

详细MSDS(安全技术说明书)

去甲氟西汀安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

去甲氟西汀文献

K2P channel gating mechanisms revealed by structures of TREK-2 and a complex with Prozac.

Science 347(6227) , 1256-9, (2015)

TREK-2 (KCNK10/K2P10), a two-pore domain potassium (K2P) channel, is gated by multiple stimuli such as stretch, fatty acids, and pH and by several drugs. However, the mechanisms that control channel g...

The pH-dependent toxicity of basic pharmaceuticals in the green algae Scenedesmus vacuolatus can be explained with a toxicokinetic ion-trapping model.

Aquat. Toxicol. 101(1) , 266-75, (2011)

Several previous studies revealed that pharmaceuticals with aliphatic amine function exhibit a higher toxicity toward algae than toward other aquatic organisms. Here we investigated the pH-dependent t...

Sequential metabolism of secondary alkyl amines to metabolic-intermediate complexes: opposing roles for the secondary hydroxylamine and primary amine metabolites of desipramine, (s)-fluoxetine, and N-desmethyldiltiazem.

Drug Metab. Dispos. 38(6) , 963-72, (2010)

Three secondary amines desipramine (DES), (S)-fluoxetine [(S)-FLX], and N-desmethyldiltiazem (MA) undergo N-hydroxylation to the corresponding secondary hydroxylamines [N-hydroxydesipramine, (S)-N-hyd...

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