Analgesic activity of a novel bivalent opioid peptide compared to morphine via different routes of administration.
Analgesic activity of a novel bivalent opioid peptide compared to morphine via different routes of administration.
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新型二价阿片肽通过不同给药途径与吗啡相比的镇痛活性。
DOI：
10.1007/bf01986590
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发表时间：
1991
期刊：
影响因子：
--
通讯作者：
Carr,DB
中科院分区：
文献类型：
--
作者：
Silbert,BS;Lipkowski,AW;Cepeda,MS;Szyfelbein,SK;Osgood,PF;Carr,DB
基于构效关系合成了一种新型二价阿片类四肽 Biphalin (Tyr-d-Ala-Gly-Phe-NH)2。与吗啡相比，在大鼠中评估了双啡林的镇痛活性。药物通过皮下 (s.c.)、静脉内 (i.v.) 和鞘内 (i.t.) 给药。使用甩尾和捏尾作为镇痛测试。 Biphalin s.c.显示出可忽略不计的镇痛活性，但静脉注射时通过这种途径产生显着的镇痛作用，但不如吗啡有效。相比之下，鞘内注射双啡肽比吗啡更有效。这些结果表明，双啡肽具有因外周酶降解或重新分布而受到损害的内在活性，这些特性可能使其可用于探索局部应用的阿片类药物在外周的镇痛作用，而不会产生不良中枢作用。
A novel bivalent opioid tetrapeptide, biphalin (Tyr-d-Ala-Gly-Phe-NH)2, was synthesized based on structure-activity relationships. The analgesic activity of biphalin was assessed in comparison to morphine in rats. Drugs were administered subcutaneously (s.c.), intravenously (i.v.) and intrathecally (i.t.). Tail flick and tail pinch were used as tests for analgesia. Biphalin s.c. showed negligible analgesic activity, but when given i.v. produced significant analgesia, although less potent than morphine via this route. In contrast, intrathecal biphalin was more potent than morphine. These results indicate that biphalin has intrinsic activity that is compromised by enzymatic degradation or redistribution in the periphery, properties that may render it useful in exploring analgesic actions of locally applied opioids in the periphery without the likelihood of unwanted central effects.