| Description | Duloxetine is an inhibitor of serotonin-norepinephrine reuptake(Ki of 4.6 nM),with treatment of major depressive disorder and generalized anxiety disorder. |
| 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]. |
| Cell experiments | 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]. |
| Target activity | 5-HT-Norepinephrine reuptake:4.6 nM(ki) |
| molecular weight | 297.41 |
| Molecular formula | C18H19NOS |
| CAS | 116539-59-4 |
| Storage | store at low temperature,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 40 mg/mL (134.49 mM), Sonication is recommended. |
| References | 1. Wang, S.Y., J. Calderon, and G. Kuo Wang, Block of neuronal Na+ channels by antidepressant duloxetine in a state-dependent manner. Anesthesiology, 2010. 113(3): p. 655-65. 2. Ekram, A, R,et al. Duloxetine in Painful Diabetic Neuropathy: A Systematic Review[J]. Clinical Journal of Pain, 2016. |