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The elmiric acids: biologically active anandamide analogs.

elmiric Acids：具有生物活性的 anandamide 类似物。

基本信息

批准号：
7727687
负责人：
SUMNER HOWARD BURSTEIN
金额：
$ 33.98万
依托单位：
UNIV OF MASSACHUSETTS MED SCH WORCESTER
依托单位国家：
美国
项目类别：
财政年份：
2009
资助国家：
美国
起止时间：
2009-08-01 至 2011-07-31
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/7727687
关键词：
Absence of pain sensation Acids Adverse effects Anabolism Analgesics Anti-Inflammatory Agents Anti-inflammatory Binding Biological Biological Models Brain Calcium ion Cannabinoids Cell Culture Techniques Cell physiology Cells Chemicals Chinese Hamster Ovary Cell Chronic inflammatory pain Data Dependence Development Endocannabinoids Enzymes Exposure to Family Family member Future Gene Silencing Glycine Inflammation Inflammatory Inhibition of Cell Proliferation Injury Intractable Pain Ligands Longevity Mass Spectrum Analysis Measures Mediating Mediator of activation protein Modeling Molecular Names Narcotics Nomenclature Orphan Pain Patients Peritoneal Fluid Pharmaceutical Preparations Physiological Population Procedures Prostaglandins Rattus Reporting Research Support Rheumatoid Arthritis Role Sampling Suggestion System Testing Time Tissues Uncertainty Work addiction analog anandamide base cannabinoid receptor capsaicin receptor cell type drug candidate glycine transporter human GPRC5C protein in vitro Model in vivo inhibitor/antagonist insight interest member receptor response

项目摘要

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.

作为化学实体，脂氨基酸已经知道一段时间了。但更多最近发现了它们在哺乳动物中的存在和重要性。他们似乎与内源性大麻素不仅在结构上，在生物行为方面。后者包括镇痛，抗炎作用，抑制细胞增殖和钙离子动员。约40个自然约会已经鉴定了该家族的发生成员，此外，还鉴定了几种合成的已经制备和研究了类似物。为了便于识别，已建议基于名称elmiric酸（EMA）。典型的例子是N-花生四烯酰甘氨酸不与CBI结合，但它确实抑制甘氨酸转运蛋白 GLYT 2a也似乎是孤儿G蛋白偶联受体GPRI 8的配体。它也可能通过其抑制作用调节组织中大麻素的水平。对FAAH的影响，FAAH是介导花生四烯酸失活的酶。中的浓度大鼠大脑中的含量是花生四烯酸的数倍，这支持了它作为一种生理介质未来的研究应旨在阐明所有的行动，这个有趣的分子家族的成员，并进一步了解可能的作用机制。这些化合物的一个有希望的用途是作为麻醉剂替代代理人。