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OBESITY RESEARCH SOLUTIONSAlrestatin is an inhibitor of aldose reductase (IC50 = 1.5 µM for rat lens enzyme).1 It is selective for rat lens aldose reductase over rat kidney aldehyde reductase (IC50 = 58 µM). 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).
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1. Inhibition of aldehyde reductase by aldose reductase inhibitors. Biochem. Pharmacol. 40(5), 1033-1042 (1990).
2. Effect of alrestatin sodium on glucose-
3. Alrestatin: Gastric acid antisecretory-