TOLRESTAT

Tolrestat is a long-acting aldose reductase inhibitor reportedly useful in the prophylaxis of diabetic neuropathy, retinopathy and cataracts.

Tolrestat is an aldose reductase inhibitor (IC₅₀ = 35 nM for the bovine lens enzyme). Dietary administration of tolrestat decreases sciatic nerve galactitol accumulation in a rat model of galactosemia (ED₅₀ = 7.3 mg/kg per day) and sciatic nerve sorbitol accumulation (ED₅₀ = 4.8 mg/kg per day) in a rat model of diabetes induced by streptozotocin (STZ; ). It also decreases urinary total protein exretion in a rat model of STZ-induced diabetes when administered at a dose of 25 mg/kg per day. Topical administration of tolrestat (2 and 3% in 10 μl four times per day) decreases levels of galactitol in the lens of and inhibits cataract formation in rats fed a high-galactose diet.

Crystallized, melting point 164-165℃. Tolrestat Methyl Ester: C17H16F3NO3S. melting point 109-110℃.

American Home Products (USA)

Alredase (Wyeth-Ayerst).

Tolrestat is an aldose reductase inhibitor.

ChEBI: Tolrestat is a member of naphthalenes. It has a role as an EC 1.1.1.21 (aldehyde reductase) inhibitor.

Alredase

Tolrestat is considered to be effective in treating the consequences of diabetes including neuropathy, nephropathy, retinopathy and esophageal motility and vibration perception. Tolrestat is also believed to have lesser or no toxic effects.

[1] KAZIMIR SESTANJ. N-[[5-(Trifluoromethyl)-6-methoxy-1-naphthalenyl]thioxomethyl]-N-methylglycine (Tolrestat), a potent, orally active aldose reductase inhibitor[J]. Journal of Medicinal Chemistry, 1984, 27 3: 255-256. DOI: 10.1021/jm00369a003
[2] M L MCCALEB. Intervention with the aldose reductase inhibitor, tolrestat, in renal and retinal lesions of streptozotocin-diabetic rats.[J]. Diabetologia, 1991, 34 10: 695-701. DOI: 10.1007/bf00401513
[3] STEFANIA BANDITELLI . A New Approach Against Sugar Cataract Through Aldose Reductase Inhibitors[J]. Experimental eye research, 1999, 69 5: Pages 533-538. DOI: 10.1006/exer.1999.0729