The elmiric acids: biologically active anandamide analogs.

elmiric Acids：具有生物活性的 anandamide 类似物。

• 批准号: 7894890
• 负责人: SUMNER HOWARD BURSTEIN
• 金额: $ 32.43万
• 依托单位: UNIV OF MASSACHUSETTS MED SCH WORCESTER
• 依托单位国家: 美国
• 财政年份: 2009
• 资助国家: 美国
• 起止时间: 2009-08-01 至 2012-01-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7894890
• 关键词: 2-arachidonylglycerol; Abbreviations; Absence of pain sensation; Acids; Acute; Adverse effects; Air; Amidohydrolases; Anabolism; Anti-Inflammatory Agents; Anti-inflammatory; Applications Grants; Binding; Biological; Biological Assay; Biological Models; Brain; CNR1 gene; Calcium ion; Cannabinoids; Categories; Cell Culture Techniques; Cell physiology; Cells; Chemical Structure; Chemicals; Chinese Hamster Ovary Cell; Chronic; Communities; Data; Dependency; Drug usage; Endocannabinoids; Enzyme-Linked Immunosorbent Assay; Enzymes; Exposure to; Family; Family member; Fibroblasts; Future; Gene Silencing; Glycine; Goals; Hydrolysis; Immunoassay; In Vitro; Inflammation; Inflammatory; Inflammatory Response; Inhibition of Cell Proliferation; Injury; Interleukin-6; Interleukins; Ligands; Link; Lipopolysaccharides; Lipoxygenase; Liquid substance; Mass Spectrum Analysis; Measures; Mediating; Mediator of activation protein; Medical; Modeling; Molecular; Mus; N-arachidonylglycine; Names; Narcotics; Nomenclature; Non-Steroidal Anti-Inflammatory Agents; Nuclear; Orphan; Pain; Peritoneal Fluid; Peritonitis; Pharmaceutical Preparations; Physiological; Platelet Activating Factor; Procedures; Prostaglandin-Endoperoxide Synthase; Prostaglandins; Rattus; Reporting; Research Support; Rheumatoid Arthritis; Risk; Role; Sampling; Scintillation Counting; Structure-Activity Relationship; Suggestion; Synovial Cell; System; TNF gene; TRPV1 gene; Testing; Tetrahydrocannabinol; Thioglycolates; Time; Tissues; Tumor Necrosis Factor-alpha; Tumor Necrosis Factors; Work; addiction; ajulemic acid; amidase; analog; anandamide; base; capsaicin receptor; cytokine; falls; fatty acid amide hydrolase; follow-up; gamma-Aminobutyric Acid; gamma-Linolenic Acid; glycine transporter; human GPRC5C protein; in vitro Model; in vivo; inhibitor/antagonist; innovation; insight; interest; member; monocyte; novel; peripheral blood; progesterone 11-hemisuccinate-(2-iodohistamine); receptor; research study; response; subcutaneous

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，脂氨基酸已知已有一段时间了。然而，更多 最近，人们发现了它们在哺乳动物物种中的出现和重要性。他们 似乎不仅在结构上而且在结构上与内源性大麻素有密切的关系 从生物作用来看。后者包括镇痛、抗炎作用、 抑制细胞增殖和钙离子动员。迄今为止自然约40 该家族的出现成员已被鉴定，此外，还有一些合成的 类似物已被制备和研究。为了便于识别，命名系统 已根据名称 elmiric Acid (EMA) 提出建议。原型示例 N-花生四烯酰甘氨酸不与 CBI 结合，但它会抑制甘氨酸转运蛋白 GLYT2a 似乎也是孤儿 G 蛋白偶联受体 GPRI8 的配体。 由于其抑制作用，它还可能在调节 anandamide 的组织水平方面发挥作用。 对介导 anandamide 失活的 FAAH 酶的影响。其浓度在 大鼠大脑比 anandamide 高几倍，支持其可能作为 生理介质。未来的研究应该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 行动机制。这些化合物的一个有前景的用途是用作麻醉剂 替代代理。