- 英文名称
- Ranirestat
- 分子式
- C17H11BrFN3O4
- 分子量
- 420.19
- 中文别名
- (R)-2'-(4-溴-2-氟苄基)-1'H-螺[吡咯烷-3,4'-吡咯并[1,2-a]吡嗪]-1',2,3',5(3'H)-四酮; AS-3201; SX-3201; AS 3201; (3R)-2'-[(4-bromo-2-fluorophenyl)methyl]spiro[pyrrolidine-3,4'-pyrrolo[1,2-a]pyrazine]-1',2,3',5-tetrone; (3R)-2'-(4-bromo-2-fluorobenzyl)spiro[pyrrolidin-3,4'(1'H)-pyrrolo[1,2-a]pyrazin]-1',2,3',5(2'H)-tetraone; (R)-2-(4-bromo-2-fluorobenzyl)spiro[1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-4,3'-pyrrolidine]-1,2',3,5'-tetrone; R-(-)-2-(4-bromo-2-fluorobenzyl)-1,2,3,4-tetrahydro[1,2-a]pyrrolopyridine-4-spiro-3'-pyrrolidine-1,2',3'5'-tetraone; SX-3202; (3R)-2'-(4-bromo-2-fluorobenzyl)spiro[pyrrolidine-3,4'(1'H)-pyrrolo[1,2-a]pyrazine]-1',2,3',5(2H')-tetraone; SX 3030
- 用途
- - 生物活性
Ranirestat (AS-3201) 是一种有效的，口服活性的醛糖还原酶 (AR) 抑制剂，对大鼠晶状体 AR 和重组人 AR 的 IC50 分别为 11 nM 和 15 nM，对于重组人 AR 的 Ki 为 0.38 nM。Ranirestat 可用于糖尿病感觉运动性多发性神经病的研究，并且对糖尿病视网膜具有神经保护作用。
- 靶点
IC50: 11 nM (Rat lens aldose reductase) and 15 nM (Recombinant humanaldose reductase)
Ki: 0.38 nM (Recombinant humanaldose reductase)
- 体外研究
Ranirestat concentration-dependently inhibits sorbitol accumulation in rat erythrocytes and sciatic nerves incubated in the high concentration (500 mg/dl) of glucose. The potency of Ranirestat inhibition of sorbitol accumulation is similar between rat erythrocytes and sciatic nerves with IC
50
values of 0.010 μM and 0.041 μM, respectively.
- 体内研究
Ranirestat (0.03-1.0 mg/kg; oral administration; once daily; for 3 weeks; male STD-Wistar rats) treatment dose-dependently decreases the elevated sorbitol and fructose levels in the rat sciatic nerves without affecting blood glucose level. Ranirestat also improves the STZ-induced decrease in motor nerve conduction velocity (MNCV) in a dose-dependent manner.
Animal Model:
Male STD-Wistar rats aged about (12-week-old; 260-290 g) injected with Streptozotocin (STZ)
Dosage:
0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg
Administration:
Oral administration; once daily; for 3 weeks
Result:
Dose-dependently decreased the elevated sorbitol and fructose levels in the rat sciatic nerves without affecting blood glucose level.
