Gorelov P I, Ostrovskaia R U, Sazonova N M
Eksp Klin Farmakol. 2013;76(7):3-5.
The effect of dipeptidal neurotensine mimetic, N-caproyl-L-prolyl-L-tyrosine methyl ester (GZR-123, Dilept) and its main metabolite N-caproyl-L-prolyl-L-tyrosine (GZR-125) was evaluated at novel objects recognition test (NOR) in the male outbred rats. NOR was chosen from many cognitive test as those involving the selective action on the attention and episodic memory and considering as translational model for the study of cognition deficiency in schizophrenics. M-cholinoblocking agent scopolamine (0.2 mg/kg s.c.) was used as agent disturbing the performance of the test. Dilept (2 mg/kp i.p.) was shown to restore the NOR performance, disturbed by scopolamine. The same was true for GZR-125 (2 mg/kp i.p.), whose cholinopositive effect could contribute to the procognitive effect of the parent molecule.
在雄性远交系大鼠的新物体识别测试(NOR)中,评估了二肽类神经降压素模拟物N-己酰基-L-脯氨酰-L-酪氨酸甲酯(GZR-123,Dilept)及其主要代谢产物N-己酰基-L-脯氨酰-L-酪氨酸(GZR-125)的作用。在众多认知测试中选择了NOR,因为它涉及对注意力和情景记忆的选择性作用,并被视为研究精神分裂症认知缺陷的转化模型。使用M胆碱阻断剂东莨菪碱(0.2 mg/kg皮下注射)作为干扰测试表现的药物。结果显示,Dilept(2 mg/kp腹腔注射)可恢复被东莨菪碱干扰的NOR表现。GZR-125(2 mg/kp腹腔注射)也是如此,其胆碱能阳性作用可能有助于母体分子的促认知作用。