Dapoxetine hydrochloride, also known as “Priligy” is a synthetic high affinity KV4.3 and KV1.5 blocker and is also a competitive 5-HT re-uptake inhibitor. Dapoxetine hydrochloride has an effective concentration of 5-300 μM with an IC50 of 5.3 and 11.6 μM on cloned KV4.3 and KV1.5 channels respectively. Dapoxetine reduces the peak amplitude of KV4.3 currents and also accelerates the decay rate of current inactivation in a concentration-dependent manner. The block of the KV4.3 channel by dapoxetine is highly voltage-dependent at a membrane potential coinciding with the activation of the channel. Dapoxetine blocks KV4.3 currents by binding to the open state of the channels and by accelerating the closed-state inactivation. Until recently it was believed that most of Dapoxetine’s (and other SSRI’s) pharmacological activity are attributed to 5-HT reuptake inhibition. This effect is used for the management of (GAD) general anxiety disorder, obesity, neuropathic pain, premature ejaculation and other medical conditions. However, lately, it has been hypothesized that Dapoxetine’s therapeutic effect is also achieved through interaction with other types of channels as well including KV type channels
产品描述
A Blocker of KV4.3 and KV1.5 Channels and an Inhibitor of 5-HT Re-Uptake
