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In vitro and in viv...
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Diao, XingxingNIDA, MD 21224 USA
(författare)
In vitro and in vivo human metabolism of a new synthetic cannabinoid NM-2201 (CBL-2201)
- Artikel/kapitelEngelska2017
Förlag, utgivningsår, omfång ...
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2016-07-06
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SPRINGER,2017
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printrdacarrier
Nummerbeteckningar
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LIBRIS-ID:oai:DiVA.org:liu-134491
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https://urn.kb.se/resolve?urn=urn:nbn:se:liu:diva-134491URI
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https://doi.org/10.1007/s11419-016-0326-9DOI
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Språk:engelska
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Sammanfattning på:engelska
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Ämneskategori:ref swepub-contenttype
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Ämneskategori:art swepub-publicationtype
Anmärkningar
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Funding Agencies|Intramural Research Program of the National Institute on Drug Abuse, National Institutes of Health
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In 2014, NM-2201 (CBL-2201), a novel synthetic cannabinoid (SC), was detected by scientists at Russian and US laboratories. It has been already added to the list of scheduled drugs in Japan, Sweden and Germany. Unfortunately, no human metabolism data are currently available, which makes it challenging to confirm its intake, especially given that all SCs investigated thus far have been found to be extensively metabolized. The present study aims to recommend appropriate marker metabolites by investigating NM-2201 metabolism in human hepatocytes, and to confirm the results in authentic human urine specimens. For the metabolic stability assay, 1 A mu M NM-2201 was incubated in human liver microsomes (HLMs) for up to 1 h; for metabolite profiling, 10 A mu M of NM-2201 was incubated in human hepatocytes for 3 h. Two authentic urine specimens from NM-2201-positive cases were subjected to beta-glucuronidase hydrolysis prior to analysis. The identification of metabolites in hepatocyte samples and urine specimens was achieved with high-resolution mass spectrometry via information-dependent acquisition. NM-2201 was quickly metabolized in HLMs, with an 8.0-min half-life. In human hepatocyte incubation samples, a total of 13 NM-2201 metabolites were identified, generated mainly from ester hydrolysis and further hydroxylation, oxidative defluorination and subsequent glucuronidation. M13 (5-fluoro PB-22 3-carboxyindole) was found to be the major metabolite. In the urine specimens, the parent drug NM-2201 was not detected; M13 was the predominant metabolite after beta-glucuronidase hydrolysis. Therefore, based on the results of our study, we recommend M13 as a suitable urinary marker metabolite for confirming NM-2201 and/or 5F-PB-22 intake.
Ämnesord och genrebeteckningar
Biuppslag (personer, institutioner, konferenser, titlar ...)
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Carlier, JeremyNIDA, MD 21224 USA
(författare)
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Zhu, MingsheBristol Myers Squibb, NJ 08543 USA
(författare)
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Pang, ShaokunSCIEX Ltd, CA 94065 USA
(författare)
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Kronstrand, RobertLinköpings universitet,Avdelningen för läkemedelsforskning,Medicinska fakulteten,National Board Forens Med, Department Forens Genet and Forens Toxicol, S-58758 Linkoping, Sweden(Swepub:liu)robkr41
(författare)
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Scheidweiler, Karl B.NIDA, MD 21224 USA
(författare)
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Huestis, Marilyn A.NIDA, MD 21224 USA; University of Maryland, MD 21224 USA
(författare)
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NIDA, MD 21224 USABristol Myers Squibb, NJ 08543 USA
(creator_code:org_t)
Sammanhörande titlar
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Ingår i:Forensic Toxicology: SPRINGER35:1, s. 20-321860-89651860-8973
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