The elmiric acids: biologically active anandamide analogs.
The elmiric acids: biologically active anandamide analogs.
批准号:
7727687
负责人:
SUMNER HOWARD BURSTEIN
金额:
$33.98万
依托单位国家:
美国
项目类别:
财政年份:
2009
资助国家:
美国
项目状态:
已结题
起止时间:
2009-08-01 至 2011-07-31
关键词:
Absence of pain sensationAcidsAdverse effectsAnabolismAnalgesicsAnti-Inflammatory AgentsAnti-inflammatoryBindingBiologicalBiological ModelsBrainCalcium ionCannabinoidsCell Culture TechniquesCell physiologyCellsChemicalsChinese Hamster Ovary CellChronic inflammatory painDataDependenceDevelopmentEndocannabinoidsEnzymesExposure toFamilyFamily memberFutureGene SilencingGlycineInflammationInflammatoryInhibition of Cell ProliferationInjuryIntractable PainLigandsLongevityMass Spectrum AnalysisMeasuresMediatingMediator of activation proteinModelingMolecularNamesNarcoticsNomenclatureOrphanPainPatientsPeritoneal FluidPharmaceutical PreparationsPhysiologicalPopulationProceduresProstaglandinsRattusReportingResearch SupportRheumatoid ArthritisRoleSamplingSuggestionSystemTestingTimeTissuesUncertaintyWorkaddictionanaloganandamidebasecannabinoid receptorcapsaicin receptorcell typedrug candidateglycine transporterhuman GPRC5C proteinin vitro Modelin vivoinhibitor/antagonistinsightinterestmemberreceptorresponse
中文摘要
作为化学实体,脂氨基酸已经知道了一段时间。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
大鼠大脑的含量比大麻素高出数倍,支持其可能的作用
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
行动机制。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。
英文摘要
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.
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The elmiric acids: biologically active anandamide analogs.
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批准号:7894890
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项目类别:
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资助金额:$32.43万
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财政年份:2009
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负责人:SUMNER HOWARD BURSTEIN
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Endocannabinoid Analogs as Anti-inflammatory Agents
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财政年份:2004
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负责人:SUMNER HOWARD BURSTEIN
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依托单位:
Endocannabinoid Analogs as Anti-inflammatory Agents
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依托单位:
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依托单位:
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负责人:SUMNER HOWARD BURSTEIN
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依托单位:
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项目类别:
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