[CAS NO. 116539-59-4]  Duloxetine

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PRODUCTS SPECIFICATIONS [116539-59-4]

Store
Catalog
SLK-S5071
Brand
Selleck
CAS
116539-59-4

DESCRIPTION [116539-59-4]

Overview

MDL-
Molecular Weight297.41
Molecular FormulaC18H19NOS
SMILESO([C@@H](CCNC)C1=CC=CS1)C=2C3=C(C=CC2)C=CC=C3

For research use only.

Storage

2 years -20°C liquid
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

Duloxetine (LY-248686) is a potent inhibitor of in vitro and in vivo and is 3- to 5-times more effective at inhibiting 5-HT uptake.

Targets

serotonin reuptake [1]norepinephrine reuptake [1]

In vitro

Duloxetine is a potent inhibitor of serotonin (5-HT) and norepinephrine reuptake. Compared with its effects on 5-HT and norepinephrine reuptake, duloxetine weakly inhibits dopamine reuptake and has low binding affinity for other neurotransmitter receptors, including adrenergic, muscarinic (nonselective) and histamine H1 receptors; dopamine D2 receptors; 5-HT1A, 5-HT1D and 5-HT2C receptors; and opioid receptors. In vitro studies showed that more than 90% of duloxetine is protein bound in human plasma. The binding occurs primarily to albumin and a1-acid glycoprotein.

In vivo

Duloxetine achieves a maximum plasma concentration (Cmax) of approximately 47 ng/mL (40mg twice-daily dosing) to 110 ng/mL (80 mg twice-daily dosing) approximately 6 hours after dosing. The elimination half-life of duloxetine is approximately 10–12 hours and the volume of distribution is approximately 1640 L. The absolute oral bioavailability averaged 50%, ranging from 30% to 80%, after a 60 mg single dose in one study and averaged 43%, ranging from 19% to 71%, in another study. Food and time of day impact duloxetine absorption, with food and bedtime administration delaying tmax by 4 hours.


Synonyms

2-Thiophenepropanamine, N-methyl-γ-(1-naphthalenyloxy)-, (γS)-
2-Thiophenepropanamine, N-methyl-γ-(1-naphthalenyloxy)-, (S)-
S)-N-Methyl-γ-(1-naphthalenyloxy)-2-thiophenepropanamine
LY 248686
Duloxetine
(S)-Duloxetine
(S)-(+)-N-Methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine
(S)-N-Methyl-3-(naphthalen-1-yloxy)-3-(thiophen-2-yl)propan-1-amine
(+)-Duloxetine
2-Thiophenepropanamine N-methyl-γ-(1-naphthalenyloxy)-, (γS)-
Ariclaim
Nodetrip
Xeristar