| Title |
In vitro and in vivo human metabolism of a new synthetic cannabinoid NM-2201 (CBL-2201)
|
|---|---|
| Published in |
Forensic Toxicology, July 2016
|
| DOI | 10.1007/s11419-016-0326-9 |
| Pubmed ID | |
| Authors |
Xingxing Diao, Jeremy Carlier, Mingshe Zhu, Shaokun Pang, Robert Kronstrand, Karl B. Scheidweiler, Marilyn A. Huestis |
| Abstract |
In 2014, NM-2201 (CBL-2201), a novel synthetic cannabinoid (SC), was detected by Russian and United States laboratories. It was already added to the scheduled drugs list in Japan, Sweden and Germany. Unfortunately, no human metabolism data are currently available, making it challenging to confirm its intake because all previous investigated SCs were extensively metabolized. The present study aims to recommend appropriate marker metabolites by investigating NM-2201 metabolism in human hepatocytes and confirm the results in authentic human urine specimens. For the metabolic stability assay, 1 μM NM-2201 was incubated in human liver microsomes (HLMs) for up to 1 h; for metabolite profiling, 10 μM of NM-2201 was incubated in human hepatocytes for 3 h. Two authentic urine specimens from NM-2201 positive cases were analyzed after β-glucuronidase hydrolysis. Metabolite identification 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 thirteen 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 the major metabolite. In the urine specimens, the parent drug NM-2201 was not detected; M13 was the predominant metabolite after β-glucuronidase hydrolysis. Therefore, based on our study, we recommend the M13 as a suitable urinary marker metabolite for confirming NM-2201 and/or 5F-PB-22 intake. |
X Demographics
The data shown below were collected from the profiles of 3 X users who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Spain | 1 | 33% |
| Portugal | 1 | 33% |
| United States | 1 | 33% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 3 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 24 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 24 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 5 | 21% |
| Student > Master | 4 | 17% |
| Researcher | 3 | 13% |
| Student > Bachelor | 2 | 8% |
| Other | 2 | 8% |
| Other | 6 | 25% |
| Unknown | 2 | 8% |
| Readers by discipline | Count | As % |
|---|---|---|
| Pharmacology, Toxicology and Pharmaceutical Science | 8 | 33% |
| Biochemistry, Genetics and Molecular Biology | 2 | 8% |
| Agricultural and Biological Sciences | 2 | 8% |
| Chemistry | 2 | 8% |
| Environmental Science | 1 | 4% |
| Other | 4 | 17% |
| Unknown | 5 | 21% |
Attention Score in Context
This research output has an Altmetric Attention Score of 5. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 12 February 2018.
All research outputs
#7,018,408
of 25,789,020 outputs
Outputs from Forensic Toxicology
#85
of 414 outputs
Outputs of similar age
#107,783
of 372,304 outputs
Outputs of similar age from Forensic Toxicology
#4
of 14 outputs
Altmetric has tracked 25,789,020 research outputs across all sources so far. This one has received more attention than most of these and is in the 72nd percentile.
So far Altmetric has tracked 414 research outputs from this source. They receive a mean Attention Score of 3.9. This one has done well, scoring higher than 78% of its peers.
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We're also able to compare this research output to 14 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 71% of its contemporaries.