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，脂肪氨基酸已经闻名了一段时间。但是，更多最近发现它们在哺乳动物物种中的发生和重要性。他们似乎与内源性大麻素有着密切的关系在生物行为方面。后者包括镇痛，抗炎作用，抑制细胞增殖和钙离子动员。迄今为止大约40天自然已经确定了这个家庭的成员，此外还有几个合成已经准备好模拟并研究了类似物。为了促进其身份，术语系统已经根据名称Elmiric Acid（EMA）提出了建议。原型示例N-芳基烯烯甘氨酸不与CBI结合，但是它确实抑制了甘氨酸转运蛋白 Glyt2a，似乎也是孤儿G蛋白偶联受体GPRI8的配体。它也可能在调节组织水平的武anandamide抑制作用中起作用对法族的影响，介导anandamide的失活的酶。它的集中度老鼠大脑比Anandamide高出几倍，支持其作为一个可能的作用生理调解人。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，并进一步了解可能作用机理。这些化合物的有希望的用途将是麻醉品替代剂。