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Gliquidone(AR-DF26)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Gliquidone(AR-DF26)图片
CAS NO:33342-05-1
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)527.63
FormulaC27H33N3O6S
CAS No.33342-05-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 105 mg/mL (199.0 mM)
Water: <1 mg/mL
Ethanol: 6 mg/mL (11.4 mM)
Solubility (In vivo)2% DMSO+Corn oil: 5mg/mL
Synonyms

Synonym: Gliquidone; Glurenorm; Beglynor; Glikvidon; Glycvidon; Sanofi Synthelabo brand of gliquidone; Yamanouchi brand of gliquidone; AR-DF 26

IUPAC/Chemical Name: 1-cyclohexyl-3-[4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxoisoquinolin-2-yl)ethyl]phenyl]sulfonylurea

InChi Key: LLJFMFZYVVLQKT-UHFFFAOYSA-N

InChi Code: InChI=1S/C27H33N3O6S/c1-27(2)23-14-11-20(36-3)17-22(23)24(31)30(25(27)32)16-15-18-9-12-21(13-10-18)37(34,35)29-26(33)28-19-7-5-4-6-8-19/h9-14,17,19H,4-8,15-16H2,1-3H3,(H2,28,29,33)

SMILES Code: CC1(C2=C(C=C(C=C2)OC)C(=O)N(C1=O)CCC3=CC=C(C=C3)S(=O)(=O)NC(=O)NC4CCCCC4)C

实验参考方法
In Vitro

In vitro activity: 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.

In VivoGliquidone (0.1–1.0 μg per mouse i.c.v.) prevents antinociception produced by amitriptyline and clomipramine in a dose-dependent manner in male swiss albino mice. Gliquidone (0.06–16 μg per mouse, i.c.v.) antagonizes the antinociception induced by buprenorphine, morphine and methadone. Gliquidone (6 μg per mouse, i.c.v.) prevents the antinociception induced by clonidine (0.125 mg/kg, s.c.) and guanabenz (0.30 mg/kg, s.c.), while a lower dose of gliquidone (3 μg per mouse, i.c.v.) is ineffective. Glurenorm (10 mg/kg) given to the diabetic rats produces significant reductions in blood glucose, nonenzymatic glycosylation, and total protein in the lenses, and significantly increases in glutathione levels in the lenses.
Animal modelMice
Formulation & Dosage10 mg/kg
References

Fundam Clin Pharmacol. 1991;5(2):107-15; Neuropharmacology. 2001;40(1):75-84; Br J Pharmacol. 1995 Mar;114(6):1296-302.