Gliquidone (Synonyms: AR-DF 26) |
Catalog No.GC16561 |
La gliquidona (AR-DF 26) es un fÁrmaco antidiabético de la clase de las sulfonilureas, utilizado en el tratamiento de la diabetes mellitus tipo 2.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 33342-05-1
Sample solution is provided at 25 µL, 10mM.
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].
References:
[1]. Ocaña M, Del Pozo E, Baeyens JM. Gliquidone, an ATP-dependent K+ channel antagonist, antagonizes morphine-induced hypermotility. Eur J Pharmacol, 1993, 239(1-3): 253-255.
[2]. Ocaña M, Baeyens JM. Role of ATP-sensitive K+ channels in antinociception induced by R-PIA, an adenosine A1 receptor agonist. Naunyn Schmiedebergs Arch Pharmacol, 1994, 350(1): 57-62.
[3]. von Nicolai H, Brickl R, Eschey H, et al. Duration of action and pharmacokinetics of the oral antidiabetic drug gliquidone in patients with non-insulin-dependent (type 2) diabetes mellitus. Arzneimittelforschung, 1997, 47(3): 247-252.
[4]. Tuerk TR, Bandur S, Nuernberger J, et al. Gliquidone therapy of new-onset diabetes mellitus after kidney transplantation. Clin Nephrol, 2008, 70(1): 26-32.
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