Norfluoxetine Hydrochloride

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CAS NO:

57226-68-3

Norfluoxetine hydrochloride 是 Fluoxetine 的 N-去甲基化活性代谢物。Fluoxetine 是一种选择性血清素 (5-HT) 再摄取抑制剂，可通过细胞色素 P450 (CYP) 2D6、CYP2C19 和 CYP3A4 代谢为 Norfluoxetine hydrochloride。Norfluoxetine hydrochloride 抑制5-HT摄取并抑制CaV3.3 T电流 (IC50=5 μM)。Norfluoxetine hydrochloride 具有抗惊厥活性。

生物活性

Norfluoxetine hydrochloride is an active N-demethylated metabolite of Fluoxetine. Fluoxetine is a selective serotonin (5-HT) reuptake inhibitor that is metabolized to Norfluoxetine hydrochloride bycytochrome P450(CYP) 2D6, CYP2C19, and CYP3A4. Norfluoxetine hydrochloride inhibits5-HTuptake and inhibitsCaV3.3 Tcurrent (IC50 = 5 μM). Norfluoxetine hydrochloride has anticonvulsant activity^[1]^[2]^[3]^[4].

IC₅₀& Target^[1]

5-HT Receptor

Ca_V3.3

5 μM (IC₅₀)

体内研究
(In Vivo)

Pretreatment with Fluoxetine or Norfluoxetine hydrochloride (20mg/kg s.c.), as well as Phenytoin (30 mg/kg s.c.) and Clonazepam (0.1mg/kg s.c.) significantly increases both the rate and duration of survival, demonstrating a significant protective effect against Pentylenetetrazol-induced epilepsy^[1].

分子量

331.76

Formula

C₁₆H₁₇ClF₃NO

CAS 号

57226-68-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.