(S)-Duloxetine hydrochloride is a high affinity KV4.3 blocker and is also a competitive inhibitor of 5-HT and NE re-uptake. Duloxetine hydrochloride has an effective concentration of 1-300 μM with an IC50 of 8.4 μM on cloned KV4.3 channels. Duloxetine is widely used for the treatment of Major Depressive disorder (MDD) through the inhibition of 5-HT and NE re-uptake. Duloxetine is generally well tolerated by patients compared to other anti-depressants with relatively mild side-effects such as- nausea, dry mouth and fatigue being the most common. Duloxetine is also used for other psychological conditions such as the treatment of general anxiety disorder (GAD) and stress related urinary incontinence where, according to one study, Duloxetine managed to increase the quality of life (I-QOL) of these patients far better than the placebo treatment. In diabetic patients suffering from associated peripheral neuropathic pain, Duloxetine was found to alleviate a 24-hour average pain evaluated on an 11-point Likert scale.
产品描述
A Blocker of KV4.3 and an Inhibitor of 5-HT and Norepinephrine (NE) Re-Uptake
产品形式
KV4 channels complexes, also known as Shal-type K+ channels are expressed in a variety of tissue, with particularly high levels in the brain and heart. These channels are the primary subunits that contribute to transient, voltage-dependent K+ currents in the nervous system and the heart. These complexes are composed of pore-forming voltage-gated α-subunits (Shal/Kv4) and at least two classes of auxiliary β-subunits- KChIPs (K+-Channel-Interacting-Proteins) and DPLPs (Dipeptidyl-Peptidase-Like-Proteins).
