| Name | Duloxetine |
| Description | Duloxetine is an inhibitor of serotonin-norepinephrine reuptake(Ki of 4.6 nM),with treatment of major depressive disorder and generalized anxiety disorder. |
| Cell Research | Used the whole cell, patch clamp technique to test whether duloxetine interacts with the neuronal Nav1.7 Na+ channel as a potential target.?Resting and inactivated Nav1.7 Na+ channel block by duloxetine were measured by conventional pulse protocols in transfected human embryonic kidney cells.?The open-channel block was determined directly using inactivation-deficient mutant Nav1.7 Na+ channels[1]. |
| In vitro | IC50 of duloxetine for the resting and inactivated wild-type hNav1.7 Na+ channel were 22.1+/-0.4 and 1.79+/-0.10 microM, respectively (mean+/-SE, n=5).?The IC50 for the open Na+ channel was 0.25+/-0.02 microM (n=5), as determined by the block of persistent late Nav1.7 Na+ currents.?Similar open-channel block by duloxetine was found in the muscle Nav1.4 isoform (IC50=0.51+/-0.05 microM;?n=5).?Block by duloxetine appeared via the conserved local anesthetic receptor as determined by site-directed mutagenesis.?Finally, duloxetine elicited strong use-dependent block of neuronal transient Nav1.7 Na+ currents during repetitive stimulations[1]. |
| Storage | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 40 mg/mL (134.49 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween-80+45% Saline : 4 mg/mL (13.45 mM), Sonication is recommended.
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| Keywords | SLC6A4 | SERT | SerotoninTransporter | serotonin-norepinephrine reuptake | Serotonin Transporter | pain | osteoarthiritis | musculoskeletal | LY-248686 | LY248686 | LY 248686 | Inhibitor | inhibit | generalized | Duloxetine | disorder | depressive | anxiety | 5-HTT | (S)-Duloxetine |
| Inhibitors Related | Dapoxetine hydrochloride | Fluvoxamine maleate | Venlafaxine hydrochloride | Desvenlafaxine succinate hydrate | 1-(2-Methoxyphenyl)piperazine hydrochloride | Amitriptyline hydrochloride | Vortioxetine hydrobromide | Trazodone hydrochloride | Fluoxetine hydrochloride | Paroxetine hydrochloride | Cinchonidine | Paroxetine |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Pain-Related Compound Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max |
United States
