| CAS NO: | 33342-05-1 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| Molecular Weight (MW) | 527.63 |
|---|---|
| Formula | C27H33N3O6S |
| 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 |
| 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 Vivo | Gliquidone (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 model | Mice |
| Formulation & Dosage | 10 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. |
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