Norfluoxetine (hydrochloride)

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 by cytochrome P450 (CYP) 2D6, CYP2C19, and CYP3A4. Norfluoxetine hydrochloride inhibits 5-HT uptake and inhibits CaV3.3 T current (IC50 = 5 μM) . Norfluoxetine hydrochloride has anticonvulsant activity[1][2][3][4].

Product Specifications

CAS Number

[57226-68-3]

UNSPSC

12352005

Hazard Statement

H302, H317, H318, H334, H336, H361, H362, H373, H410

Target

5-HT Receptor; Calcium Channel; Drug Metabolite

Type

Reference compound

Related Pathways

GPCR/G Protein; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/norfluoxetine-hydrochloride.html

Purity

99.58

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

FC(F)(F)C1=CC=C(OC(C2=CC=CC=C2)CCN)C=C1.Cl

Molecular Formula

C16H17ClF3NO

Molecular Weight

331.76

Precautions

H302, H317, H318, H334, H336, H361, H362, H373, H410

References & Citations

[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.