Eight Met- and Leu-enkephalin analogs substituted with L- or D-Arg at position 2 were synthesized using NG-mesitylene-2-sulfonylarginine. Among them, H-Tyr-D-Arg-Gly-Phe-Met-OH was found to possess an analgesic effect 2.4 times higher than that of morphine on a molar basis, when injected intracisternally. This compound was also found to produce analgesia when administered intravenously.
合成了八个在第2位分别用L-或
D-精氨酸取代的甲
硫脑啡肽和亮
脑啡肽类似物,所用原料为NG-间
甲苯-2-磺酰精
氨酸。在鞘内注射时,发现其中的H-Tyr-D-Arg-Gly-Phe-Met-OH具有比
吗啡高2.4倍的镇痛作用(摩尔比)。该化合物经静脉给药时也能产生镇痛作用。