Home Neuronal Signaling Serotonin Transporter inhibitor - 5-HT Receptor inhibitor Duloxetine For research use only.

Duloxetine

Synonyms: LY-248686

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.

Duloxetine Chemical Structure

Duloxetine Chemical Structure

CAS No. 116539-59-4

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Duloxetine Related Products

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
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
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].

Chemical Information & Solubility

Molecular Weight 297.41 Formula

C18H19NOS
CAS No. 116539-59-4 SDF --
Density 1.158 g/mL
Smiles CNCCC(C1=CC=CS1)OC2=CC=CC3=CC=CC=C32
Storage (From the date of receipt) 2 years -20°C liquid

In vitro
Batch:

DMSO : 59 mg/mL ( (198.37 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 59 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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