Annelies Cannaert
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View article: Machine Learning to Assist in Large-Scale, Activity-Based Synthetic Cannabinoid Receptor Agonist Screening of Serum Samples
Machine Learning to Assist in Large-Scale, Activity-Based Synthetic Cannabinoid Receptor Agonist Screening of Serum Samples Open
Background Synthetic cannabinoid receptor agonists (SCRAs) are amongst the largest groups of new psychoactive substances (NPS). Their often high activity at the CB1 cannabinoid receptor frequently results in intoxication, imposing serious …
View article: Are the <i>N</i>‐demethylated metabolites of U‐47700 more active than their parent compound? In vitro μ‐opioid receptor activation of <i>N</i>‐desmethyl‐U‐47700 and <i>N</i>,<i>N</i>‐bisdesmethyl‐U‐47700
Are the <i>N</i>‐demethylated metabolites of U‐47700 more active than their parent compound? In vitro μ‐opioid receptor activation of <i>N</i>‐desmethyl‐U‐47700 and <i>N</i>,<i>N</i>‐bisdesmethyl‐U‐47700 Open
Studies on the tissue distribution of the new synthetic opioid U‐47700 and its main metabolite N ‐desmethyl‐U‐47700 revealed about sixfold higher metabolite concentrations in pig brain as compared with the parent compound. To better assess…
View article: Systematic evaluation of a panel of 30 synthetic cannabinoid receptor agonists structurally related to MMB‐4en‐PICA, MDMB‐4en‐PINACA, ADB‐4en‐PINACA, and MMB‐4CN‐BUTINACA using a combination of binding and different CB1 receptor activation assays. Part III: The G protein pathway and critical comparison of different assays
Systematic evaluation of a panel of 30 synthetic cannabinoid receptor agonists structurally related to MMB‐4en‐PICA, MDMB‐4en‐PINACA, ADB‐4en‐PINACA, and MMB‐4CN‐BUTINACA using a combination of binding and different CB1 receptor activation assays. Part III: The G protein pathway and critical comparison of different assays Open
The present work is the last of a three‐part study investigating a panel of 30 systematically designed synthetic cannabinoid receptor agonists (SCRAs) including features such as the 4‐pentenyl tail and varying head groups including amides …
View article: Shape matters: The application of activity‐based <i>in vitro</i> bioassays and chiral profiling to the pharmacological evaluation of synthetic cannabinoid receptor agonists in drug‐infused papers seized in prisons
Shape matters: The application of activity‐based <i>in vitro</i> bioassays and chiral profiling to the pharmacological evaluation of synthetic cannabinoid receptor agonists in drug‐infused papers seized in prisons Open
Synthetic cannabinoid receptor agonists (SCRAs) elicit many of their psychoactive effects via type‐1 human cannabinoid (CB 1 ) receptors. Enantiomer pairs of eight tert ‐leucinate or valinate indole‐ and indazole‐3‐carboxamide SCRAs were s…
View article: First Report on Brorphine: The Next Opioid on the Deadly New Psychoactive Substance Horizon?
First Report on Brorphine: The Next Opioid on the Deadly New Psychoactive Substance Horizon? Open
New psychoactive substances continue to appear on the drug market. Until recently, new synthetic opioids, which are among the most dangerous new psychoactive substances, primarily encompassed analogs of the potent analgesic fentanyl. Latel…
View article: Report on a New Opioid NPS: Chemical and <i>In Vitro</i> Functional Characterization of a Structural Isomer of the MT-45 Derivative Diphenpipenol
Report on a New Opioid NPS: Chemical and <i>In Vitro</i> Functional Characterization of a Structural Isomer of the MT-45 Derivative Diphenpipenol Open
In this paper, the identification and full characterization of a novel non-fentanyl opioid sourced online, which is a member of the 1-substituted-4-(1,2-diphenylethyl)piperazine derivatives related to MT-45, is reported. The sample was sol…
View article: <i>In vitro</i> activity profiling of Cumyl‐PEGACLONE variants at the CB<sub>1</sub> receptor: Fluorination <i>versus</i> isomer exploration
<i>In vitro</i> activity profiling of Cumyl‐PEGACLONE variants at the CB<sub>1</sub> receptor: Fluorination <i>versus</i> isomer exploration Open
Synthetic cannabinoid receptor agonists (SCRAs) are one of the largest groups of new psychoactive substances monitored in Europe. SCRAs are known to typically exert higher cannabinoid activity than tetrahydrocannabinol from cannabis, there…
View article: Report on a novel emerging class of highly potent benzimidazole NPS opioids: Chemical and in vitro functional characterization of isotonitazene
Report on a novel emerging class of highly potent benzimidazole NPS opioids: Chemical and in vitro functional characterization of isotonitazene Open
This paper reports on the identification and full chemical characterization of isotonitazene ( N , N ‐diethyl‐2‐[5‐nitro‐2‐({4‐[(propan‐2‐yl)oxy]phenyl}methyl)‐1H‐benzimidazol‐1‐yl]ethan‐1‐amine), a potent NPS opioid and the first member o…
View article: Hide and Seek: Overcoming the Masking Effect of Opioid Antagonists in Activity-Based Screening Tests
Hide and Seek: Overcoming the Masking Effect of Opioid Antagonists in Activity-Based Screening Tests Open
To the Editor:
We previously reported on an alternative activity-based screening method to detect (synthetic) opioids/opiates in blood samples (1) in which μ-opioid receptor activation could be monitored via a split-luciferase system. The…
View article: Enantiospecific Synthesis, Chiral Separation, and Biological Activity of Four Indazole-3-Carboxamide-Type Synthetic Cannabinoid Receptor Agonists and Their Detection in Seized Drug Samples
Enantiospecific Synthesis, Chiral Separation, and Biological Activity of Four Indazole-3-Carboxamide-Type Synthetic Cannabinoid Receptor Agonists and Their Detection in Seized Drug Samples Open
Synthetic cannabinoid receptor agonists (SCRAs) have been the largest group of illicit psychoactive substances reported to international monitoring and early warning systems for many years. Carboxamide-type SCRAs are amongst the most preva…
View article: Functional evaluation of carboxy metabolites of synthetic cannabinoid receptor agonists featuring scaffolds based on L‐valine or L‐<i>tert</i>‐leucine
Functional evaluation of carboxy metabolites of synthetic cannabinoid receptor agonists featuring scaffolds based on L‐valine or L‐<i>tert</i>‐leucine Open
Indole‐ and indazole‐based synthetic cannabinoid receptor agonists (SCRAs), featuring valine or tert ‐leucine substituents, are commonly abused new psychoactive substances (NPS). A major metabolic pathway for these SCRAs is hydrolysis of t…
View article: Validation of Activity-Based Screening for Synthetic Cannabinoid Receptor Agonists in a Large Set of Serum Samples
Validation of Activity-Based Screening for Synthetic Cannabinoid Receptor Agonists in a Large Set of Serum Samples Open
We previously reported an alternative screening method for the detection of synthetic cannabinoid receptor agonists (SCRAs)1 in serum and plasma samples (1). SCRAs are one of the largest groups of new psychoactive substances (NPS) worldwid…
View article: Activity-Based Detection and Bioanalytical Confirmation of a Fatal Carfentanil Intoxication
Activity-Based Detection and Bioanalytical Confirmation of a Fatal Carfentanil Intoxication Open
Carfentanil, one of the most potent opioids known, has recently been reported as a contaminant in street heroin in the United States and Europe, and is associated with an increased number of life-threatening emergency department admissions…
View article: Activity-Based Detection of Consumption of Synthetic Cannabinoids in Authentic Urine Samples Using a Stable Cannabinoid Reporter System
Activity-Based Detection of Consumption of Synthetic Cannabinoids in Authentic Urine Samples Using a Stable Cannabinoid Reporter System Open
Synthetic cannabinoids (SCs) continue to be the largest group of new psychoactive substances (NPS) monitored by the European Monitoring Center of Drugs and Drugs of Abuse (EMCDDA). The identification and subsequent prohibition of single SC…
View article: Detection and Activity Profiling of Synthetic Cannabinoids and Their Metabolites with a Newly Developed Bioassay
Detection and Activity Profiling of Synthetic Cannabinoids and Their Metabolites with a Newly Developed Bioassay Open
Synthetic cannabinoids (SCs) are the largest group of compounds currently monitored in Europe by the EU Early Warning System on new psychoactive substances. Emerging recreational use of these products has led to multiple cases of adverse h…