Duloxetine 是一种 5 羟色胺-去甲肾上腺素重吸收 (serotonin-Norepinephrine reuptake) 抑制剂，Ki=4.6 nM，可作用于广泛性焦虑症的研究。

Duloxetine is an inhibitor of serotonin-norepinephrine reuptake(Ki of 4.6 nM),with treatment of major depressive disorder and generalized anxiety disorder.

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].

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].

116539-59-4

C18H19NOS

297.42

DMSO:15mg/mL(50.4 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years