ArticleArchives of toxicology2025
Dipyanone, a new methadone-like synthetic opioid: In vitro and in vivo human metabolism and pharmacological profiling.
Article in Archives of toxicology, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 citing papers in PubMed.
- Phase I metabolism of the methadone analog methiodone (IC-26) in pooled human liver microsomes and its detection in seven authentic human cases.Archives of toxicology · 2026Article
- Phase I Metabolism of Novel Phencyclidine Derivative 3-Cl-PCP: In Vitro Studies With Pooled Human Liver Microsomes and Investigation of a Post-Mortem Case.Drug testing and analysis · 2026Article
- Investigation of the In Vitro and In Vivo Metabolism and μ-Opioid Receptor Affinity of the Nitazene N-Pyrrolidino Fluetonitazene.Drug testing and analysis · 2026Article
- Human metabolism and pharmacological profiling of protonitazepyne and metonitazepyne, two highly potent nitazenes: prediction of main metabolite activity based on µ-opioid receptor docking simulations.Archives of toxicology · 2026Article
- In Silico Forensic Toxicology: Is It Feasible?Toxics · 2025Review
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Authors and funding
9 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The emergence of novel synthetic opioids (NSOs) poses significant challenges to public health, toxicologists, and law enforcement. Since the comprehensive scheduling of fentanyl analogues in many countries worldwide, several non-fentanyl NSOs have emerged on the illicit drug market, increasing the risks of addiction and fatal overdoses. Dipyanone, a methadone-like NSO, was first identified in drug seizures in 2021 and later also in postmortem cases. This study aimed to assess the metabolism of dipyanone in humans using in silico predictions, in vitro human hepatocyte incubations, and authentic urine specimens. Dipyanone was primarily metabolised through the opening of the pyrrolidine ring to form the corresponding N-butan-4-ol or N-butanoic acid compound, followed by cyclisation to 4'-[2-ethylidene-5-methyl-3,3-diphenylpyrrolidin-1-yl]butan-1'-ol (EMDPB) and 4'-[2-ethylidene-5-methyl-3,3-diphenylpyrrolidin-1-yl]butanoic acid (EMDPBA); other metabolic transformations included hydroxylation, reduction, and O-glucuronidation. We propose EMDPB and EMDPBA as specific biomarkers of dipyanone consumption. Additionally, dipyanone's activation of µ- (MOR), κ- (KOR), and δ- (DOR) opioid receptors was evaluated with a homogeneous time-resolved fluorescence-based GTP G
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