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对内吗啡肽(endomorphins, EMs)和合理替换其2-/3-位氨基酸(amino acid, Aa)而得到的8个类似物进行了受体结合作用、 镇痛活性和舒血管效应研究, 探讨了EMs的构效关系. 结果表明: 相对而言, 2-Aa与EMs的选择性更相关, 而3-Aa则与其亲和性更相关; EMs及其类似物的镇痛和舒血管效应不完全由它们的受体结合作用(in vitro)所决定, [D-Pro2]EM-2作用独特; EMs在中枢系统中的镇痛作用和在循环系统中的舒血管作用的失活机制是不同的, 前者可能与降解有关, 而后者可能与反馈抑制有关.
Receptor binding, analgesic activity and vasodilator effects of eight analogs derived from endomorphins (EMs) and rational replacement of 2- / 3- amino acids (Aa) were investigated. The results showed that 2-Aa was more related to the selectivity of EMs, while 3-Aa was more related to its affinity. The analgesic and vasodilator effects of EMs and its analogues were not Because of their receptor binding (in vitro), [D-Pro2] EM-2 acts uniquely; the mechanism of analgesic action of EMs in the central nervous system and the mechanism of inactivation of vasodilatation in the circulatory system are different , The former may be related to degradation, while the latter may be related to feedback inhibition.