In vitro and in vivo metabolism and detection of 3-HO-PCP, a synthetic phencyclidine, in human samples and pooled human hepatocytes using high resolution mass spectrometry.

@article{Davidsen2020InVA,
  title={In vitro and in vivo metabolism and detection of 3-HO-PCP, a synthetic phencyclidine, in human samples and pooled human hepatocytes using high resolution mass spectrometry.},
  author={Anders Bork Davidsen and Marie Mardal and Sys Stybe Johansen and Petur Weihe Dalsgaard and Kristian Linnet},
  journal={Drug testing and analysis},
  year={2020}
}
The new psychoactive substance (NPS) 3-HO-PCP, a phencyclidine (PCP) analogue, was detected in a law enforcement seizure and in forensic samples in Denmark. Compared to PCP, 3-HO-PCP is known to be a more potent dissociative NPS, but no toxicokinetic investigations of 3-HO-PCP are yet available. Therefore, 3-HO-PCP was quantified in in vivo samples, and the following were investigated: plasma protein binding, in vitro and in vivo metabolites and metabolic targets. All samples were separated by… 

References

SHOWING 1-10 OF 30 REFERENCES
In Vitro Metabolism and Hepatic Intrinsic Clearance of the Synthetic Cannabinoid Receptor Agonist JWH-122 and Its Four ω-Halogenated Analogues
TLDR
In vitro ω-halogenation with larger halogens appears to increase the intrinsic hepatic stability, thereby prolonging exposure and possibly the duration of action.
Metabolites to parent 3-MeO-PCP ratio in human urine collected in two fatal cases.
TLDR
It is concluded that testing for 3-MeO-PCP metabolites does not increase the window of detection of the drug, and the ratio between metabolites and parent 3- MeO- PCP, always lower than 1, were calculated to estimate the proportionality of metabolites.
Syntheses, analytical and pharmacological characterizations of the 'legal high' 4-[1-(3-methoxyphenyl)cyclohexyl]morpholine (3-MeO-PCMo) and analogues.
TLDR
3-Me-PCMo was found to have moderate affinity for NMDAR comparable to that of ketamine, and had an approximate 12-fold lower affinity than PCP, which supports the anecdotal reports of dissociative effects from 3-MeO-PC Mo in humans.
Analytical strategy to investigate 3,4-methylenedioxypyrovalerone (MDPV) metabolites in consumers’ urine by high-resolution mass spectrometry
TLDR
The potential of high-resolution mass spectrometry for the investigation of human in vivo metabolism of 3,4-methylenedioxypyrovalerone using urine collected from a consumer using non-controlled experiments and several compounds identified have not been previously reported in the literature are investigated.
Predictive value of animal models for human cytochrome P450 (CYP)-mediated metabolism: A comparative study in vitro
TLDR
If hepatic xenobiotic-metabolizing characteristics were to be the sole reason for the selection of animal species for toxicity studies, then the rat might not be the most appropriate model to mimic human CYP activity patterns.
Phencyclidine analog use in Sweden—intoxication cases involving 3-MeO-PCP and 4-MeO-PCP from the STRIDA project
TLDR
Clinical and bioanalytical data from analytically confirmed non-fatal intoxications associated with 3- and/or 4-MeO-PCP within the STRIDA project constitute an important basis for the assessment of NPS hazard and availability.
Phencyclidine disposition after intravenous and oral doses
TLDR
PCP comprised 16% of urinary radioactivity with 31% consisting of enzymatically hydrolyzable conjugates of hydroxylated metabolites and both cis and trans isomers of 4‐phenyl‐4‐(1‐piperidinyl)cyclohexanol were found.
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