【摘要】 目的 通过离体活性实验来研究morphiceptin中苯丙氨酸的角色。方法 通过豚鼠回肠纵行肌(GPI)实验和小鼠输精管(MVD)实验鉴定所有化合物的离体活性。结果 实验表明在morphiceptin的3位引入Hfe或者4位引入Phg能够较好的模拟Phe的作用，D-Phg则效果不佳。结论 morphiceptin的3位和4位的芳环在受体结合中所扮演的角色是不同的。

    【关键词】 Mophiceptin；苯丙氨酸模拟物；阿片受体；离体生物检定

    In vitro activities of phenylalanine mimics substituted analogues of morphiceptin

    【Abstract】 Aim To study the role of phenylalanine in morphiceptin by in vitro bioassay. Methods Their in vitro activities were determined on guinea pig ileum and mouse vas deference. Results In vitro bioassay data showed that introducing Hfe into position 3 or Phg into position 4 could mimic the role of phenylalanine well. D-Phg could not mimic the role of phenylalanine. Conclusion The role of receptor binding for the aromatic group in positon 3 was different from that of position 4.

    【Key words】 Morphiceptin; Phenylalanine mimics; Opioid receptors; In vitro bioassay

    Morphiceptin(Mcp)是1981年由Chang等在对牛奶蛋白β-casein中的一个七肽片断β-casomorphin的类似物改造中合成出来的一个对μ阿片受体具有较高亲和性和选择性的四肽 ......