Literature DB >> 26641707

In vitro metabolism of a novel synthetic cannabinoid, EAM-2201, in human liver microsomes and human recombinant cytochrome P450s.

Ju Hyun Kim1, Hee Seung Kim2, Tae Yeon Kong1, Joo Young Lee1, Jin Young Kim2, Moon Kyo In2, Hye Suk Lee3.   

Abstract

In vitro metabolism of a new synthetic cannabinoid, EAM-2201, has been investigated with human liver microsomes and major cDNA-expressed cytochrome P450 (CYP) isozymes using liquid chromatography-high resolution mass spectrometry (LC-HRMS). Incubation of EAM-2201 with human liver microsomes in the presence of NADPH resulted in the formation of 37 metabolites, including nine hydroxy-EAM-2201 (M1-M9), five dihydroxy-EAM-2201 (M10-M14), dihydrodiol-EAM-2201 (M15), oxidative defluorinated EAM-2201 (M16), two hydroxy-M16 (M17 and M18), three dihydroxy-M16 (M19-M21), N-dealkyl-EAM-2201 (M22), two hydroxy-M22 (M23 and M24), dihydroxy-M22 (M25), EAM-2201 N-pentanoic acid (M26), hydroxy-M26 (M27), dehydro-EAM-2201 (M28), hydroxy-M28 (M29), seven dihydroxy-M28 (M30-M36), and oxidative defluorinated hydroxy-M28 (M37). Multiple CYPs, including CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2J2, 3A4, and 3A5, were involved in the metabolism of EAM-2201. In conclusion, EAM-2201 is extensively metabolized by CYPs and its metabolites can be used as an indicator of EAM-2201 abuse.
Copyright © 2015 Elsevier B.V. All rights reserved.

Entities:  

Keywords:  Cytochrome P450; EAM-2201; Human liver microsomes; In vitro metabolism; LC–HRMS; Synthetic cannabinoid

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Substances：

Year:  2015        PMID： 26641707     DOI： 10.1016/j.jpba.2015.11.023

Source DB:  PubMed          Journal:  J Pharm Biomed Anal        ISSN： 0731-7085            Impact factor:   3.935


  5 in total

1.  In Vitro Inhibitory Effects of Synthetic Cannabinoid EAM-2201 on Cytochrome P450 and UDP-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes.

Authors:  Tae Yeon Kong; Soon-Sang Kwon; Jae Chul Cheong; Hee Seung Kim; Jin Young Kim; Hye Suk Lee
Journal:  Molecules       Date:  2018-04-16       Impact factor: 4.411

2.  Severe Vitamin K-dependent Coagulopathy from Rodenticide-contaminated Synthetic Cannabinoids: Emergency Department Presentations.

Authors:  Erik Wright; John W Hafner; Gregory Podolej; Douglas L Feinstein; Richard van Breemen; Israel Rubinstein; Steven Aks; Michael Wahl
Journal:  West J Emerg Med       Date:  2021-07-15

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Journal:  Front Pharmacol       Date:  2022-03-10       Impact factor: 5.810

4.  Inhibitory Effect of Lygodium Root on the Cytochrome P450 3A Enzyme in vitro and in vivo.

Authors:  Yunfang Zhou; Ailian Hua; Quan Zhou; Peiwu Geng; Feifei Chen; Lianhe Yan; Shuanghu Wang; Congcong Wen
Journal:  Drug Des Devel Ther       Date:  2020-05-19       Impact factor: 4.162

5.  In vitro metabolism of synthetic cannabinoid AM1220 by human liver microsomes and Cunninghamella elegans using liquid chromatography coupled with high resolution mass spectrometry.

Authors:  Shimpei Watanabe; Unnikrishnan Kuzhiumparambil; Shanlin Fu
Journal:  Forensic Toxicol       Date:  2018-05-24       Impact factor: 4.096
  5 in total

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