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An increase in phosphorylated GSK-3 β in a rat kidney tissue was observed 1 h after i/p injection of LiCl or dalagrin. Prolonged gentamicin 6-days injection caused a nephrotoxic effect leading to AKI manifested by increased blood creatinine and urea levels. I/p injection of dalargin or LiCl 3 h before gentamicin injection led to drop of these levels thus improving renal function after gentamicin treatment. After 3 h of gentamicin treatment we observed a profound ROS production in kidney vital slices while after LiCl or dalargin pretreatment ROS levels were much lower. Histological analysis of rat kidneys affected by gentamicin revealed significant necrosis of proximal tubular epithelium with intense granular degeneration. After dalargin treatment, morphological features of gentamicin-induced nephropathy were less obvious. The most remarkable recovering effects on a histological level were observed after LiCl treatment. Analyses of cultured renal tubular cells survival have revealed that cells death reached 90% at 5 mg/ml of gentamycin. Pretreatment for 1 h with 100 μg/ml of dalargin or 3 mM LiCl essentially rescued cultured renal cells from gentamycin-induced cell death.