Synthesis and pharmacological activity of analogs of the endogenous neuropeptide cycloprolylglycine
Synthesis and pharmacological activity of analogs of the endogenous neuropeptide cycloprolylglycine
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DOI：
10.1007/s11094-012-0741-0
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发表时间：
2012-05-01
影响因子：
0.9
通讯作者：
Gudasheva, T. A.
中科院分区：
文献类型：
--
作者：
Kolyasnikova, K. N.;Vichuzhanin, M. V.;Gudasheva, T. A.
合成了一系列内源性环丙氨酰甘氨酸的类似物和同系物。在电击或东莨菪碱诱发失忆的被动回避实验模型上，研究了合成化合物的促进性。采用高架正迷宫实验检测其抗焦虑活性。已经证实，负责催产素和抗焦虑活性的药效团是不同的。提出了关于结合区结构和相应药理靶点的假设。
A series of analogs and homologs of the endogenous cyclic dipeptide cycloprolylglycine were synthesized. The nootropic properties of the synthesized compounds were investigated on an experimental model of a passive avoidance test with electroshock- or scopolamine-induced amnesia. The anxiolytic activity was examined by an elevated plus-maze test. It is established that the pharmacophores responsible for the nootropic and anxiolytic activities are different. Hypotheses concerning the structure of the binding regions with the corresponding pharmacological targets are formulated.