Alrestatin is an inhibitor of aldose reductase (IC50 = 1.5 ?M for rat lens enzyme).1 It is selective for rat lens aldose reductase over rat kidney aldehyde reductase (IC50 = 58 ?M). Alrestatin reduces basal and tyramine-induced norepinephrine release in rat pancreatic preparations.2 In vivo, alrestatin (0.75 mmol/kg) increases plasma insulin levels in fasted anesthetized rats. Alrestatin inhibits the lens and sciatic nerve accumulation of polyols in a rat model of streptozotocin-induced diabetes.3 It also inhibits gastric acid secretion and ulcer formation induced by pyloric ligation in rats (ED50s = 90 and 330 mg/kg, respectively).
1.Sato, S., and Kador, P.F.Inhibition of aldehyde reductase by aldose reductase inhibitorsBiochem. Pharmacol.40(5)1033-1042(1990) 2.Kobric, M., and Lippmann, W.Effect of alrestatin sodium on glucose-stimulated insulin secretion in the fasted anaesthetized ratHorm. Metab. Res.10(6)495-500(1978) 3.Lippmann, W., Seethaler, K., Borella, L.E., et al.Alrestatin: Gastric acid antisecretory-antiulcer activity in the ratDigestion18(1-2)35-44(1978)