Duloxetine Chemical Properties
- Boiling point:466.2±40.0 °C(Predicted)
- Density 1.158±0.06 g/cm3(Predicted)
- EPA Substance Registry System2-Thiophenepropanamine, N-methyl-?-(1-naphthalenyloxy)-, (?S)- (116539-59-4)
- Hazardous Substances Data116539-59-4(Hazardous Substances Data)
Duloxetine Usage And Synthesis
- brand nameCymbalta (Lilly).
- General DescriptionDuloxetine (Cymbalta) is a newer antidepressant. It islargely like venlafaxine, which is an SNERI (selective norepinephrinereuptake inhibitor).
- PharmacokineticsDuloxetine appears to be fairly well absorbed after oral doses, with peak plasma levels in 6 to 10 hours and
linear pharmacokinetics. The drug is extensively metabolized in the liver to active
metabolites, with 72% of an oral dose primarily excreted in the urine as conjugated metabolites and up to
15% appearing in the feces.
N-demethylation to an active metabolite (CYP2D6) and hydroxylation of the naphthyl ring (CYP1A2) at either the 4-, 5-, or 6-positions are the main metabolic pathways for duloxetine. Its metabolites are primarily excreted into the urine as glucuronide, sulfate, and O-methylated conjugation products. The major metabolites found in plasma also were found in the urine. Preclinical data for 4-hydroxyduloxetine suggests it has a similar pharmacological profile to duloxetine, with selective inhibition of SERT but less activity at the NET.
- Clinical UseDuloxetine has been approved for the treatment of depression and diabetic peripheral neuropathic pain. It is another analogue in the line of fluoxetine-based products from Lilly, in which the phenyl and phenoxy groups of fluoxetine have been respectively replaced with the benzene isostere, thiophene, and a naphthyloxy group (previously described under fluoxetine). Duloxetine exhibits dual inhibition with high affinity for the SERTs and NETs, with a five times preferential inhibition of the SERT. Duloxetine appears to be a more potent in vitro blocker of SERTs and NETs than venlafaxine. In humans, duloxetine has a low affinity for the other neuroreceptors, suggesting low incidence of unwanted adverse effects.
Duloxetine Preparation Products And Raw materials
- Raw materialsFluoronaphthalene
- Paroxetine (r)-duloxetine,R-DULOXETINE HCL,(r)-n-methyl-gama-(1-naphthalenyloxy)-2-thiophenepropanamine N-METHYL DULOXETINE-NAPHTHYL-D7 Duloxetine-naphthyl-D7 Maleate DULOXETINE HCL PELLETS Duloxetine intermediate Duloxetine intermediate AA Duloxetine hydrochoride (rs)-duloxetine hydrochloride,(rs)-n-methyl-gama-(1-naphthalenyloxy)-2-thiophenepropanamine hydrochloride 4-Hydroxy duloxetine glucuronide Duloxetine-d3 HCl R-DULOXETINE HYDROCHLORIDE (S)-(+)-N,N-Dimethyl-3-(1-naphthalenyloxy)-3-(2-thienyl)propanamine DULOXETINE-NAPHTHYL-D7 5-Hydroxy-6-methoxy duloxetine sulfate 4-Hydroxy Duloxetine 4-Hydroxy Duloxetine -D-Glucuronide,4-Hydroxy Duloxetine b-D-Glucuronide S-(+)-N,N-DIMETHYL-3-(1-NAPHTHLENYLOXY)-3-(2-THIENYL)-PROPANAMINE
- Company Name:3B Pharmachem (Wuhan) International Co.,Ltd.
- Tel:18930552037 821-50328103-801
- Company Name:LGM Pharma
- Company Name:Shanghai Longsheng chemical Co.,Ltd.
- Tel:13585536065 021-58099652-8005
- Company Name:China Langchem Inc.
- Company Name:Hunan Hui Bai Shi Biotechnology Co., Ltd.
- Tel:13308453923 0731-85529965-