Source:http://linkedlifedata.com/resource/pubmed/id/17110113
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2006-12-15
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pubmed:abstractText |
2-Arachidonoylglycerol (2-AG (1)) is an endogenous ligand for the cannabinoid receptors (CB1 and CB2). There is growing evidence that 2-arachidonoylglycerol plays important physiological and pathophysiological roles in various mammalian tissues and cells, though the details remain to be clarified. In this study, we synthesized several remarkable analogs of 2-arachidonoylglycerol, closely related in chemical structure to 2-arachidonoylglycerol: an analog containing an isomer of arachidonic acid with migrated olefins (2-AGA118 (3)), an analog containing a one-carbon shortened fatty acyl moiety (2-AGA113 (4)), an analog containing an one-carbon elongated fatty acyl moiety (2-AGA114 (5)), a hydroxy group-containing analog (2-AGA105 (6)), a ketone group-containing analog (2-AGA109 (7)), and a methylene-linked analog (2-AGA104 (8)). We evaluated their biological activities as cannabinoid receptor agonists using NG108-15 cells which express the CB1 receptor and HL-60 cells which express the CB2 receptor. Notably, these structural analogs of 2-arachidonoylglycerol exhibited only weak agonistic activities toward either the CB1 receptor or the CB2 receptor, which is in good contrast to 2-arachidonoylglycerol which acted as a full agonist at these cannabinoid receptors. These results clearly indicate that the structure of 2-arachidonoylglycerol is strictly recognized by the cannabinoid receptors (CB1 and CB2) and provide further evidence that the cannabinoid receptors are primarily the intrinsic receptors for 2-arachidonoylglycerol.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/2-arachidonylglycerol,
http://linkedlifedata.com/resource/pubmed/chemical/Arachidonic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Glycerides,
http://linkedlifedata.com/resource/pubmed/chemical/Indicators and Reagents,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Cannabinoid, CB1,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Cannabinoid, CB2,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Cannabinoid
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0968-0896
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
15
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
854-67
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pubmed:meshHeading |
pubmed-meshheading:17110113-Arachidonic Acids,
pubmed-meshheading:17110113-Cell Line,
pubmed-meshheading:17110113-Glycerides,
pubmed-meshheading:17110113-HL-60 Cells,
pubmed-meshheading:17110113-Humans,
pubmed-meshheading:17110113-Indicators and Reagents,
pubmed-meshheading:17110113-Ligands,
pubmed-meshheading:17110113-Receptor, Cannabinoid, CB1,
pubmed-meshheading:17110113-Receptor, Cannabinoid, CB2,
pubmed-meshheading:17110113-Receptors, Cannabinoid,
pubmed-meshheading:17110113-Structure-Activity Relationship
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pubmed:year |
2007
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pubmed:articleTitle |
Synthesis and biological evaluation of several structural analogs of 2-arachidonoylglycerol, an endogenous cannabinoid receptor ligand.
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pubmed:affiliation |
Department of Pharmaceutical Chemistry, Faculty of Pharmcaceutical Sciences, Teikyo University, Sagamihara, Kanagawa 199-0195, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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