Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
22
pubmed:dateCreated
2008-11-10
pubmed:abstractText
The structure-activity relationships of organophosphorus (OP) and organosulfur compounds were examined in vitro and in vivo as inhibitors of mouse brain monoacylglycerol lipase (MAGL) hydrolysis of 2-arachidonoylglycerol (2-AG) and agonist binding at the CB1 receptor. Several compounds showed exceptional potency toward MAGL activity with IC(50) values of 0.1-10 nM in vitro and high inhibition at 10mg/kg intraperitoneally in mice. We find for the first time that MAGL activity is a major in vivo determinant of 2-AG and arachidonic acid levels not only in brain but also in spleen, lung, and liver. Apparent direct OP inhibition of CB1 agonist binding may be due instead to metabolic stabilization of 2-AG in brain membranes as the actual inhibitor.
pubmed:grant
pubmed:commentsCorrections
http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-10945879, http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-11470906, http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-12518029, http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-12944586, http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-14595399, http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-16310817, http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-16449251, http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-17257165, http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-17353660, http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-17979719, http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-18096503, http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-18292184, http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-18420277, http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-18429637, http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-18438404, http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-7575630, http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-7858978, http://linkedlifedata.com/resource/pubmed/commentcorrection/18752948-9037253
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Nov
pubmed:issn
1464-3405
pubmed:author
pubmed:issnType
Electronic
pubmed:day
15
pubmed:volume
18
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
5875-8
pubmed:dateRevised
2010-12-28
pubmed:meshHeading
pubmed:year
2008
pubmed:articleTitle
Monoacylglycerol lipase regulates 2-arachidonoylglycerol action and arachidonic acid levels.
pubmed:affiliation
Environmental Chemistry and Toxicology Laboratory, Department of Environmental Science, Policy and Management, 115 Wellman Hall, University of California, Berkeley, CA 94720-3112, USA.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't, Research Support, N.I.H., Extramural