- Jeong, I. et al. (2012) Neuropharmacol. 62, 2261.
- Alomone Labs Dapoxetine hydrochloride blocks KV4. 3 channels expressed in Xenopus oocytes.A. Time course of KV4.3 current amplitude and inhibition by 100 µM Dapoxetine hydrochloride (#D-175). Currents were elicited by application of voltage step from a holding potential of -80 mV to 0 mV (150 msec), every 10 seconds. B. Superimposed example traces of current responses before and during perfusion of 100 µM Dapoxetine hydrochloride, as indicated.
KV4 channels, also known as Shal-type K+ channels, are expressed in a variety of tissues, with particularly high levels in the brain and heart. These channels contribute to transient, voltage-dependent K+ currents in the nervous system and heart1. KV1 channels are also expressed in various tissues and are usually activated by membrane depolarization2.
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 activities are attributed to 5-HT reuptake inhibition. This effect is used for the management of General anxiety disorder (GAD), obesity, neuropathic pain, premature ejaculation and other medical conditions. It has, however, been hypothesized that Dapoxetine’s therapeutic effects are also achieved through interaction with other types of channels as well as KV type channels3.
Dapoxetine hydrochloride (#D-175) is a highly pure, synthetic, and biologically active compound.