The elmiric acids: biologically active anandamide analogs.

作为一种化学物质，脂氨基酸已被人们认识了一段时间。然而，更多 最近，它们在哺乳动物中的存在和重要性已被发现。他们 似乎不仅在结构上与内源性大麻素有密切的关系，而且在 在生物作用方面。后者包括镇痛、消炎、 抑制细胞增殖和钙离子动员。到目前为止大约有40年了 已经确定了该家族的现有成员，此外，还有几个合成的 已经制备并研究了类似物。为了方便他们的身份识别，一个命名系统 根据榄香酸(EMA)的名字提出。典型的例子，N-花生四烯酰甘氨酸不与CBI结合，但它抑制甘氨酸转运体 GLYT2a，也似乎是孤儿G蛋白偶联受体GPRI8的配体。 它还可能通过其抑制作用而调节组织中的花生胺水平。 对FAAH的影响--介导去乙酰氨基酶失活的酶。其浓度集中在 大鼠的大脑比阿南达胺高几倍，这支持了它可能作为 生理调停者。未来的研究应该旨在阐明所有人的行为 这一有趣的分子家族的成员，并获得对可能的 行动机制。这些化合物的一个很有希望的用途是作为麻醉剂 替换剂。

As chemical entities, lipoamino acids have been known for some time. However, more recently their occurrence and importance in mammalian species has been discovered. They appear to have close relationships with the endocannabinoids not only structurally but also in terms of biological actions. The latter include analgesia, anti-inflammatory effects, inhibition of cell proliferation and calcium ion mobilization. To date about 40 naturally occurring members of this family have been identified and, additionally, several synthetic analogs have been prepared and studied. To facilitate their identity, a nomenclature system has been suggested based on the name elmiric acid (EMA). The prototypic example, N-arachidonoyl glycine does not bind to CBI, however it does inhibit the glycine transporter GLYT2a and also appears to be a ligand for the orphan G-protein-coupled receptor GPRI8. It may also have a role in regulating tissue levels of anandamide by virtue of its inhibitory effect on FAAH the enzyme that mediates inactivation of anandamide. Its concentration in rat brain is several times higher than anandamide supporting its possible role as a physiological mediator. Future studies should be aimed at elucidating the actions of all of the members of this interesting family of molecules and gaining further insight into possible mechanisms of action. A promising use for these compounds would be as narcotic replacement agents.