Krueger J M, Walter J, Karnovsky M L, Chedid L, Choay J P, Lefrancier P, Lederer E
J Exp Med. 1984 Jan 1;159(1):68-76. doi: 10.1084/jem.159.1.68.
Sleep-promoting activities of muramyl dipeptide (MDP) (NAc-Mur-L-ala-D-isogln) and the naturally occurring muramyl peptide(s), factor S, have recently been demonstrated. We now have amplified our understanding of structural requirements for somnogenic activity. The effects of several analogs of MDP on rabbit slow-wave sleep are presented and these results are compared to the dose-response relationship for MDP. Some tentative conclusions as to structural requirements for somnogenic activity are presented; most notably, amidation of the free gamma-carboxyl of MDP and several of its analogs resulted in the loss of somnogenic activity. MDP also can induce febrile and immunostimulatory responses. In the present paper, we show that some analogs possess immunostimulatory and pyrogenic activity but not somnogenic activity, thus suggesting that these biological activities of muramyl peptides may, in part, be mediated by separate mechanisms.
最近已证实，胞壁酰二肽（MDP）（N-乙酰胞壁酰-L-丙氨酸-D-异谷氨酰胺）以及天然存在的胞壁酰肽（因子S）具有促进睡眠的活性。我们现在对促眠活性的结构要求有了更深入的理解。本文介绍了几种MDP类似物对兔慢波睡眠的影响，并将这些结果与MDP的剂量反应关系进行了比较。文中还给出了关于促眠活性结构要求的一些初步结论；最值得注意的是，MDP及其几种类似物的游离γ-羧基酰胺化导致促眠活性丧失。MDP还可诱导发热和免疫刺激反应。在本文中，我们表明一些类似物具有免疫刺激和致热活性，但不具有促眠活性，因此表明胞壁酰肽的这些生物学活性可能部分由不同的机制介导。
