Topics

Phenethylamine-derived new psychoactive substances 2C-E-FLY, 2C-EF-FLY, and 2C-T-7-FLY: Investigations on their metabolic fate including isoenzyme activities and their toxicological detectability in urine screenings.

08:00 EDT 12th July 2019 | BioPortfolio

Summary of "Phenethylamine-derived new psychoactive substances 2C-E-FLY, 2C-EF-FLY, and 2C-T-7-FLY: Investigations on their metabolic fate including isoenzyme activities and their toxicological detectability in urine screenings."

Psychoactive substances of the 2C-series are phenethylamine-based designer drugs that can induce psychostimulant and hallucinogenic effects. The so-called 2C-FLY series contains rigidified methoxy groups integrated in a 2,3,6,7-tetrahydrobenzo[1,2-b:4,5-b']difuran core. The aim of the presented work was to investigate the in vivo and in vitro metabolic fate including isoenzyme activities and toxicological detectability of the three new psychoactive substances (NPS) 2C-E-FLY, 2C-EF-FLY, and 2C-T-7-FLY to allow clinical and forensic toxicologists the identification of these novel compounds. Rat urine, after oral administration, and pooled human liver S9 fraction (pS9) incubations were analyzed by liquid chromatography-high-resolution tandem mass spectrometry (LC-HRMS/MS). By performing activity screenings, the human isoenzymes involved were identified and toxicological detectability in rat urine investigated using standard urine screening approaches (SUSAs) based on gas chromatography (GC)-MS, LC-MS , and LC-HRMS/MS. In total, 32 metabolites were tentatively identified. Main metabolic steps consisted of hydroxylation and N-acetylation. Phase I metabolic reactions were catalyzed by CYP2D6, 3A4, and FMO3 and N-acetylation by NAT1 and 2. Methoxyamine was used as a trapping agent for detection of the deaminated metabolite formed by MAO-A and B. Interindividual differences in the metabolism of the 2C-FLY drugs could be caused by polymorphisms of enzymes involved or drug-drug interactions. All three SUSAs were shown to be suitable to detect an intake of these NPS but common metabolites of 2C-E-FLY and 2C-EF-FLY have to be considered during interpretation of analytical findings.

Affiliation

Journal Details

This article was published in the following journal.

Name: Drug testing and analysis
ISSN: 1942-7611
Pages:

Links

DeepDyve research library

PubMed Articles [12218 Associated PubMed Articles listed on BioPortfolio]

Pharmacological profiles of compounds in preworkout supplements ("boosters").

Preworkout supplements ("boosters") are used to enhance physical and mental performance during workouts. These products may contain various chemical substances with undefined pharmacological activity....

Flexible high resolution-mass spectrometry approach for screening new psychoactive substances in urban wastewater.

The number of new psychoactive substances (NPS) on the recreational drug market has increased rapidly in the last years, creating serious challenges for public health agencies and law enforcement auth...

Differential effects of psychoactive substances on human wildtype and polymorphic T356M dopamine transporters (DAT).

Many psychoactive substances affect the human dopamine (DA) reuptake transporter (hDAT). Polymorphisms in the encoding gene could affect the functionality of the transporter and consequently alter eff...

Death cases involving certain new psychoactive substances: A review of the literature.

In the last decades, more and more new psychoactive substances (NPS) were introduced on the drug market which were sold as "legal" alternatives for classic drugs and misused medications. Due to an inc...

Rapid Detection and Validated Quantification of Psychoactive Compounds in Complex Plant Matrices by Direct Analysis in Real Time-High Resolution Mass Spectrometry - Application to "Kava" Psychoactive Pepper Products.

Classified by the UNODC as a top 20 plant of concern, Piper methysticum (also known as Kava) is being increasingly abused recreationally for its mind-altering effects. It is of significant forensic re...

Clinical Trials [5621 Associated Clinical Trials listed on BioPortfolio]

Alcohol and Other Psychoactive Substances in Road Traffic - a Case-control Study

The main purpose of the study is to determine the accident risk when driving under the influence of psychoactive substances, including alcohol (DUI). Other aims are to find out the prevale...

Musitox® Project: Consumption of Psychoactive Substances at Music Festivals in Aquitaine

Poisoning by psychoactive substances is increasingly common in Europe and can be responsible for deaths. These substances, also called "festive drugs", circulate among other places in fest...

French Study on COgnitive Enhancement and Consumption of Psychoactive Substances Among Youth Students

This descriptive and declarative study will help to find out consumption rates, all psychoactive substances taken together, among 18-25 year olds. More specifically, it will allow assessme...

Characterization of the Metabolic Fate of an Oral Arginine Form

The purpose of this study is to compare the metabolic fate of two oral forms of L-Arginine in healthy subjects featuring metabolic syndrome related risk factors

Voluntary Drug Poisoning by Psychoactive Molecules: Identify Cognitive Markers

To identify in patients admitted for Voluntary drug poisoning (IMV) by psychoactive substances, T1 predictors of T2 recall of psychiatric interview and care project.

Medical and Biotech [MESH] Definitions

Specific effects of drugs and substances on metabolic pathways such as those occurring through the CYTOCHROME P-450 ENZYME SYSTEM. These include effects that often result in DRUG INTERACTIONS; FOOD-DRUG INTERACTIONS; and HERB-DRUG INTERACTIONS.

A derivative of phenethylamine containing two substituent methoxy groups in the phenyl ring.

A collective term for nutritional disorders resulting from poor absorption or nutritional imbalance, and metabolic disorders resulting from defects in biosynthesis (ANABOLISM) or breakdown (CATABOLISM) of endogenous substances.

Drug formulations or delivery systems intended to discourage the abuse of CONTROLLED SUBSTANCES. These may include physical barriers to prevent chewing or crushing the drug; chemical barriers that prevent extraction of psychoactive ingredients; agonist-antagonist combinations to reduce euphoria associated with abuse; aversion, where controlled substances are combined with others that will produce an unpleasant effect if the patient manipulates the dosage form or exceeds the recommended dose; delivery systems that are resistant to abuse such as implants; or combinations of these methods.

Epithelial cell line originally derived from porcine kidneys. It is used for pharmacologic and metabolic studies.

Quick Search


DeepDyve research library

Relevant Topics

Urology
Benign Prostatic Hyperplasia (BPH) Erectile Dysfunction Urology Urology is the branch of medicine concerned with the urinary tract and diseases that affect it. Examples include urethritis, urethrostenosis and incontinence. Urology is a su...

Hepatology
Hepatology is the study of liver, gallbladder, biliary tree, and pancreas, and diseases associated with them. This includes viral hepatitis, alcohol damage, cirrhosis and cancer. As modern lifestyles change, with alcoholism and cancer becoming more promi...

Multiple Sclerosis MS
Multiple sclerosis (MS) is the most common disabling neurological condition affecting 100,000 young adults in the UK. The condition results from autoimmune damage to myelin, causing interference in nerve signaling. Symptoms experienced depend on the pa...


Searches Linking to this Article