In order to obtain enkephalin derivatives with high analgesic activity, four enkephalinol analogs having the Tyr-D-Arg unit in the N-terminal position were synthesized. Of these, H-Tyr-D-Arg-Gly-MePhe-Met (O)-ol exhibited analgesic activity comparable to that of morphine after intravenous administration to mice.
为了获得具有高效镇痛活性的
脑啡肽衍
生物,合成了四种在N端位置含有Tyr-D-Arg单元的
脑啡肽类似物。其中,H-Tyr-D-Arg-Gly-甲基Phe-Met (O)-ol在小鼠静脉注射后表现出与
吗啡相当的镇痛活性。