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Gliquidone is an antagonist of ATP-sensitive K+ channel with IC50 value of 27.2 nM [1].

ATP-sensitive K+ channel is a type of K+ channel that is gated by intracellular ATP and ADP. ATP-sensitive K+ channel mainly exists in plasma membrane.

Gliquidone is an ATP-sensitive K+ channel antagonist. In mice, gliquidone (10 or 40 μg) antagonized morphine (20 mg/kg) induced hypermotility in a dose-dependent way. These results suggested that ATP-sensitive K+ channels played an important role in morphine-induced hypermotility [1]. In mice, gliquidone (2-8 μg) antagonized the antinociceptive effect induced by R-PIA (the adenosine A1 receptor agonist) in a dose-dependent way, which suggested that ATP-sensitive K+ channels mediated antinociception induced by R-PIA [2].

In patients with type 2 diabetes mellitus, gliquidone reduced the mean plasma glucose levels by 15% and increased insulin levels by 40% [3]. In Caucasian patients with new-onset diabetes mellitus (NODM) after kidney transplantation, gliquidone reduced fasting blood glucose (FBG) from 154 mg/dl to 120 mg/dl [4].

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