Duloxetine

For research use only.

Catalog No.S5071 Synonyms: LY-248686

Duloxetine Chemical Structure

CAS No. 116539-59-4

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

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Biological Activity

Description Duloxetine (LY-248686) is a potent inhibitor of serotonin (5-hydroxytryptamine, 5-HT) and noradrenaline (NE) uptake 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[1].

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[1].

Protocol

Solubility (25°C)

Chemical Information

Molecular Weight 297.41
Formula

C18H19NOS

Density 1.158 g/mL
CAS No. 116539-59-4
Storage 2 years -20°C liquid
Synonyms LY-248686
Smiles CNCCC(C1=CC=CS1)OC2=CC=CC3=CC=CC=C32

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID