| Title |
Metabolic fate of desomorphine elucidated using rat urine, pooled human liver preparations, and human hepatocyte cultures as well as its detectability using standard urine screening approaches
|
|---|---|
| Published in |
Analytical & Bioanalytical Chemistry, July 2016
|
| DOI | 10.1007/s00216-016-9740-4 |
| Pubmed ID | |
| Authors |
Lilian H. J. Richter, Yeda Rumi Kaminski, Fozia Noor, Markus R. Meyer, Hans H. Maurer |
| Abstract |
Desomorphine is an opioid misused as "crocodile", a cheaper alternative to heroin. It is a crude synthesis product homemade from codeine with toxic byproducts. The aim of the present work was to investigate the metabolic fate of desomorphine in vivo using rat urine and in vitro using pooled human liver microsomes and cytosol as well as human liver cell lines (HepG2 and HepaRG) by Orbitrap-based liquid chromatography-high resolution-tandem mass spectrometry or hydrophilic interaction liquid chromatography. According to the identified metabolites, the following metabolic steps could be proposed: N-demethylation, hydroxylation at various positions, N-oxidation, glucuronidation, and sulfation. The cytochrome P450 (CYP) initial activity screening revealed CYP3A4 to be the only CYP involved in all phase I steps. UDP-glucuronyltransferase (UGT) initial activity screening showed that UGT1A1, UGT1A8, UGT1A9, UGT1A10, UGT2B4, UGT2B7, UGT2B15, and UGT2B17 formed desomorphine glucuronide. Among the tested in vitro models, HepaRG cells were identified to be the most suitable tool for prediction of human hepatic phase I and II metabolism of drugs of abuse. Finally, desomorphine (crocodile) consumption should be detectable by all standard urine screening approaches mainly via the parent compound and/or its glucuronide assuming similar kinetics in rats and humans. |
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 % |
|---|---|---|
| Unknown | 3 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 2 | 67% |
| Scientists | 1 | 33% |
Mendeley readers
The data shown below were compiled from readership statistics for 30 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 30 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 5 | 17% |
| Student > Bachelor | 4 | 13% |
| Researcher | 4 | 13% |
| Student > Master | 4 | 13% |
| Other | 2 | 7% |
| Other | 0 | 0% |
| Unknown | 11 | 37% |
| Readers by discipline | Count | As % |
|---|---|---|
| Agricultural and Biological Sciences | 6 | 20% |
| Chemistry | 5 | 17% |
| Biochemistry, Genetics and Molecular Biology | 2 | 7% |
| Medicine and Dentistry | 2 | 7% |
| Neuroscience | 1 | 3% |
| Other | 3 | 10% |
| Unknown | 11 | 37% |
Attention Score in Context
This research output has an Altmetric Attention Score of 2. 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 26 January 2018.
All research outputs
#15,739,529
of 25,373,627 outputs
Outputs from Analytical & Bioanalytical Chemistry
#4,753
of 9,619 outputs
Outputs of similar age
#209,441
of 366,074 outputs
Outputs of similar age from Analytical & Bioanalytical Chemistry
#45
of 159 outputs
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So far Altmetric has tracked 9,619 research outputs from this source. They receive a mean Attention Score of 3.1. This one is in the 48th percentile – i.e., 48% of its peers scored the same or lower than it.
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We're also able to compare this research output to 159 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 69% of its contemporaries.