| Endocannabinoid structure-activity relationships for interaction at the cannabinoid receptors. | |
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MedLine Citation:
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PMID: 12052032 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Anandamide (N -arachidonoylethanolamine) was the first ligand to be identified as an endogenous ligand of the G-protein coupled cannabinoid CB1 receptor. Subsequently, two other fatty acid ethanolamides, N -homo- gamma -linolenylethanolamine and N -7,10,13,16-docosatetraenylethanolamine were identified as endogenous cannabinoid ligands. A fatty acid ester, 2-arachidonoylglycerol (2-AG), and a fatty acid ether, 2-arachidonyl glyceryl ether also have been isolated and shown to be endogenous cannabinoid ligands. Recent studies have postulated the existence of carrier-mediated anandamide transport that is essential for termination of the biological effects of anandamide. A membrane bound amidohydrolase (fatty acid amide hydrolase, FAAH), located intracellularly, hydrolyzes and inactivates anandamide and other endogenous cannabinoids such as 2-AG. 2-AG has also been proposed to be an endogenous CB2 ligand. Structure-activity relationships (SARs) for endocannabinoid interaction with the CB receptors are currently emerging in the literature. This review considers cannabinoid receptor SAR developed to date for the endocannabinoids with emphasis upon the conformational implications for endocannabinoid recognition at the cannabinoid receptors. |
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Authors:
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Patricia H Reggio |
Publication Detail:
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Type: Journal Article; Research Support, U.S. Gov't, P.H.S.; Review |
Journal Detail:
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Title: Prostaglandins, leukotrienes, and essential fatty acids Volume: 66 ISSN: 0952-3278 ISO Abbreviation: Prostaglandins Leukot. Essent. Fatty Acids Publication Date: 2002 Feb-Mar |
Date Detail:
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Created Date: 2002-06-07 Completed Date: 2002-12-06 Revised Date: 2007-11-14 |
Medline Journal Info:
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Nlm Unique ID: 8802730 Medline TA: Prostaglandins Leukot Essent Fatty Acids Country: Scotland |
Other Details:
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Languages: eng Pagination: 143-60 Citation Subset: IM |
Copyright Information:
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Copyright 2002 Elsevier Science Ltd. All rights reserved. |
Affiliation:
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Department of Chemistry, Kennesaw State University, 1000 Chastain Road, Kennesaw, GA 30144, USA. preggio@kennesaw.edu |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Cannabinoids / chemistry, metabolism*, pharmacology* Eicosanoids / chemistry, metabolism*, pharmacology* Endocannabinoids Models, Molecular Molecular Structure Receptors, Cannabinoid Receptors, Drug / agonists, chemistry, metabolism* Structure-Activity Relationship Substrate Specificity |
| Grant Support | |
ID/Acronym/Agency:
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DA 03934/DA/NIDA NIH HHS; K02 DA 00489/DA/NIDA NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Cannabinoids; 0/Eicosanoids; 0/Endocannabinoids; 0/Receptors, Cannabinoid; 0/Receptors, Drug |
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