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Dose-Dependent Effect of Nerve Growth Factor Mimetic GK-2 in a Wistar Rat Diabetes Model
Pharmaceutical Chemistry Journal ( IF 0.9 ) Pub Date : 2021-07-24 , DOI: 10.1007/s11094-021-02420-1
S. V. Ivanov 1 , R. U. Ostrovskaya 1 , T. A. Gudasheva 1 , S. B. Seredenin 1
Affiliation  

Experimental results for the new nerve growth factor (NGF) mimetic GK-2 [bis-(N-monosuccinyl-L-glutamyl-L-lysine)hexamethylenediamide] administered perorally toWistar rats in a streptozotocin-induced type 2 diabetes mellitus model are reported. The antihyperglycemic activity of GK-2 was determined in a dose range from 1 to 10 mg/kg. The most pronounced effect was observed at doses of 2.5 and 5 mg/kg. GK-2 was also found to reduce the severity of polydipsia and polyphagia and to produce a positive effect on the body-weight dynamics of diabetic animals. The dose dependence of GK-2 effects was described by a bell-shaped curve typical of regulatory peptides with various chemical structures. The ten-fold greater width of the dose–activity curve of the drug observed in this work combined with its high safety suggests that a satisfactory therapeutic index for GK-2 as a potential antidiabetic drug for peroral administration can be expected.



中文翻译:

神经生长因子模拟物 GK-2 在 Wistar 大鼠糖尿病模型中的剂量依赖性效应

为新的神经生长因子(NGF)模拟物GK-2 [实验结果( - ñ -monosuccinyl-大号谷氨酰基大号[-赖氨酸)六亚甲基二酰胺]在链脲佐菌素诱导的 2 型糖尿病模型中向 Wistar 大鼠口服给药。GK-2 的抗高血糖活性在​​ 1 至 10 mg/kg 的剂量范围内测定。在 2.5 和 5 mg/kg 的剂量下观察到最显着的效果。还发现 GK-2 可减轻烦渴和多食的严重程度,并对糖尿病动物的体重动态产生积极影响。GK-2 效应的剂量依赖性由具有各种化学结构的调节肽的典型钟形曲线描述。在这项工作中观察到的药物剂量 - 活性曲线的十倍宽度与其高安全性相结合,表明 GK-2 作为口服给药的潜在抗糖尿病药物具有令人满意的治疗指数。

更新日期:2021-07-24
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