Giorgio Tarzia, Francesca Antonietti, Andrea Duranti, Andrea Tontini, Marco Mor, Silvia Rivara, Pietro Traldi, Giuseppe Astarita, Alvin King, Jason R. Clapper, Daniele Piomelli
{"title":"Identification of a Bioactive Impurity in a Commercial Sample of 6-Methyl-2-p-Tolylaminobenzo[d][1,3]Oxazin-4-One (URB754)","authors":"Giorgio Tarzia, Francesca Antonietti, Andrea Duranti, Andrea Tontini, Marco Mor, Silvia Rivara, Pietro Traldi, Giuseppe Astarita, Alvin King, Jason R. Clapper, Daniele Piomelli","doi":"10.1002/adic.200790073","DOIUrl":null,"url":null,"abstract":"<p>The compound URB754 was recently identified as a potent inhibitor of the endocannabinoid-deactivating enzyme monoacylglycerol lipase (MGL) by screening of a commercial chemical library. Based on HPLC/MS, NMR and EI/MS analyses, the present paper shows that the MGL-inhibitory activity attributed to URB754 is in fact due to a chemical impurity present in the commercial sample, identified as bis(methylthio)mercurane. Although this organomercurial compound is highly potent at inhibiting MGL (IC<sub>50</sub> = 11.9±1.1 nM), its biological use is prohibited by its toxicity and target promiscuity.</p>","PeriodicalId":8193,"journal":{"name":"Annali di chimica","volume":"97 9","pages":"887-894"},"PeriodicalIF":0.0000,"publicationDate":"2007-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1002/adic.200790073","citationCount":"23","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Annali di chimica","FirstCategoryId":"1085","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/adic.200790073","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 23
Abstract
The compound URB754 was recently identified as a potent inhibitor of the endocannabinoid-deactivating enzyme monoacylglycerol lipase (MGL) by screening of a commercial chemical library. Based on HPLC/MS, NMR and EI/MS analyses, the present paper shows that the MGL-inhibitory activity attributed to URB754 is in fact due to a chemical impurity present in the commercial sample, identified as bis(methylthio)mercurane. Although this organomercurial compound is highly potent at inhibiting MGL (IC50 = 11.9±1.1 nM), its biological use is prohibited by its toxicity and target promiscuity.
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