Theoretical conformational analysis of met‐enkephalin
Theoretical conformational analysis of met‐enkephalin
复制标题
甲脑啡肽的理论构象分析
DOI：
10.1016/0014-5793(77)80010-0
复制
发表时间：
1977
期刊：
影响因子：
3.5
通讯作者：
M. Koch
中科院分区：
文献类型：
--
作者：
J. Coen;C. Humblet;M. Koch
最近从哺乳动物大脑中分离出两种五肽，脑啡肽（H-Tyr-Gly-Gly-Phe-X-OH，X= Met 或 Leu）[11。随后的研究主要集中在Metenkephalin上，在本文中它与脑啡肽同义。根据生理实验假设脑啡肽是阿片受体的内源性配体。它与分离的受体结合，但尚不清楚它对这些受体的亲和力是否高于或低于吗啡，因为在类似条件下已报道亲和力比率范围为 1/20 [2] 至 3 [1]。脑啡肽是内源性阿片剂的假设已在以下事实中找到了另一个合理性：高剂量的颅内微量注射可在大鼠中产生短暂的镇痛作用 [2]。但请注意，最近分离出了一种能产生持久镇痛作用的不同肽[3]。
Two pentapeptides, enkephalins (H-Tyr-Gly-Gly-Phe-X-OH, X= Met or Leu), have recently been isolated from mammalian brain [11. Subsequent investigations have mainly concentrated on Metenkephalin which is synonymous with enkephalin in the present paper. It was assumed on the basis of physiological experiments that enkephalin is the endogenous ligand of opiate receptors. It binds to isolated receptors but it is not yet clear whether its affinity for these receptors is higher or lower than that of morphine since affinity ratios ranging from l/20 [2] to 3 [1] have been reported under similar conditions.The assumption that enkephalin is the endogenous opiate has found one more justification in the fact that intracranial microinjection of a high dose produces an evanescent analgesia in rats [2]. Note, however, that a different peptide which produces a long lasting analgesia has recently been isolated [3].