Archives of Toxicology - The Consciousness Library

The toxicity of psychedelic LSD derivatives: 1-acetyl-LSD (ALD-52), 1-propionyl-LSD (1P-LSD), 1-butyryl-LSD (1B-LSD), 1-valeryl-LSD (1V-LSD) and 1-cyclopropylmethanoyl-LSD (1cP-LSD)-prediction of toxicological parameters relevant to clinical and forensic toxicology using multi-in silico approach.

Archives of Toxicology July 1, 2026 Kamil Jurowski, Alicja Krośniak, Damian Kobylarz et al.

Lysergamide analogs such as ALD-52, 1P-LSD, 1B-LSD, 1 V-LSD, and 1cP-LSD have emerged as new psychoactive substances (NPS) with hallucinogenic potential, yet their toxicological profiles remain largely unexplored. In this study, a comprehensive in silico assessment was conducted using multiple platforms (e.g., ADMETlab 3.0, Percepta, STopTox, ProTox 3.0, VEGA, TEST 5.1.2) to predict critical...

DOI: 10.1007/s00204-025-04255-1 Full text Forensic toxicology Lysergamide analogs New psychoactive substance Toxicology in silico

Global emergence and γ-aminobutyric acid type A (GABAA) receptor activity of the new designer benzodiazepine ethylbromazolam

Archives of Toxicology May 20, 2026 Caitlyn Norman, Dean Acreman, Meera Bissram et al.

Abstract Designer benzodiazepines (DBZDs) are a class of new psychoactive substances (NPS) designed as legal alternatives to prescription BZDs. Bromazolam has been the most prevalent DBZD detected on the recreational market around the world; however, a new DBZD, ethylbromazolam (8-bromo-1-ethyl-6-phenyl-4 H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine; also known as bromoethylazolam) has recently...

DOI: 10.1007/s00204-026-04433-9 Full text Benzodiazepine Designer drug In vitro toxicology Medical prescription +8

In-silico toxicity study of tryptamine, psilocin, psilocybin, N,N-dimethyltryptamine, 5'-methoxy-N,N-dimethyltryptamine and O-acetylpsilocin.

Archives of Toxicology March 31, 2026 Kamil Jurowski, Damian Kobylarz, Maciej Noga

Understanding the toxicity of serotonergic tryptamines is becoming increasingly important from both clinical and forensic perspectives, yet experimental data for these compounds remain extremely limited. Despite their growing medical relevance and widespread non-medical use, there is still no systematic evaluation of their toxicological risks. This study presents the first comprehensive in...

DOI: 10.1007/s00204-026-04365-4 Full text In silico toxicology Computational toxicology Forensic toxicology Tryptamines

ADME profile of phencyclidine (PCP) analogues: emerging dissociative hallucinogens 3-MeO-PCP (CAS: 72242-03-6) and 4-MeO-PCP (CAS: 2201-35-6)-a multi-in silico approach for comprehensive prediction of absorption, distribution, metabolism and excretion relevant to clinical and forensic toxicology.

Archives of Toxicology January 28, 2026 Kamil Jurowski, Damian Kobylarz, Maciej Noga

A multi-platform in silico workflow was applied to characterize the ADME profile of the methoxy-substituted phencyclidines 3-MeO-PCP and 4-MeO-PCP for clinical toxicological and forensic use. Predictions from ACD/Percepta, SwissADME, pkCSM, ADMETlab 3.0, DruMAP 2.0 and XenoSite were triangulated under OECD (Q)SAR principles with explicit applicability-domain checks. Both analogues were...

DOI: 10.1007/s00204-025-04283-x Full text Adme In silico New psychoactive substance Phencyclidine +1

Qualitative and quantitative in silico toxicity profiling of "angel dust": phencyclidine (PCP) analogues as new psychoactive substances (3-HO-PCP, 3-MeO-PCP, 4-MeO-PCP, 3-HO-PCE, 3-MeO-PCE, 4-MeO-PCE).

Archives of Toxicology December 8, 2025 Maciej Noga, Kamil Jurowski

Phencyclidine (PCP), historically known as "angel dust," and its analogues (3-HO-PCP, 3-MeO-PCP, 4-MeO-PCP, 3-HO-PCE, 3-MeO-PCE, 4-MeO-PCE) are dissociative new psychoactive substances with high abuse potential and limited experimental safety data. An integrated in silico workflow (STopTox, admetSAR 3.0, ADMETlab 3.0, ACD/Labs Percepta, Toxtree, ProTox 3.0, OCHEM, TEST, VEGA QSAR) was applied...

DOI: 10.1007/s00204-025-04242-6 Full text Acute toxicity Cardiotoxicity Computational toxicology Forensic toxicology +3

Dimethyltryptamine and harmine, components of ayahuasca, prevented cocaine-induced apoptosis in SH-SY5Y human neuroblastoma cells

Archives of Toxicology November 12, 2025 Gilles Salles, Carolina Aparecida de Faria Almeida, Isabella de Carvalho Alves et al.

Ayahuasca is a psychoactive brew traditionally used in religious rituals by indigenous Amazonian populations and South American syncretic religions such as Santo Daime and União do Vegetal. Its psychoactive effects are primarily due to N,N-dimethyltryptamine (DMT), while harmine (HRE), a β-carboline alkaloid, inhibits monoamine oxidase (MAO), enabling DMT's oral bioavailability. Recent studies...

DOI: 10.1007/s00204-025-04208-8 Ayahuasca Harmine Apoptosis Flow cytometry +13

Biotransformation of ketamine in terminal in vivo experiments under chronic intermittent hypoxia conditions and the role of AhR.

Archives of Toxicology April 19, 2025 António B Pimpão, Luísa Teixeira-Santos, Nuno R Coelho et al.

We were pioneers in describing aryl hydrocarbon receptor (AhR) activation by chronic intermittent hypoxia (CIH) in a rat pre-clinical model. This model mimics hypertension (HTN) secondary to obstructive sleep apnea, enabling longitudinal investigation of hypertension development. Concerns about the influence of barbiturates on AhR-regulated enzymes led us to opt for ketamine/medetomidine...

DOI: 10.1007/s00204-025-04044-w Full text Aryl hydrocarbon receptor Hydroxynorketamine Norketamine glucuronide Obstructive sleep apnea +4

Metabolism study of two phenethylamine - derived new psychoactive substances using in silico, in vivo, and in vitro approaches.

Archives of Toxicology March 10, 2025 Yiling Tang, Linhao Xu, Zhenshuo Guo et al. 1 citation

New psychoactive substances (NPS) are substances that are not controlled by international drug control conventions but are abused and pose a threat to public health. Proscaline and methallylescaline are two phenylethylamines with psychoactive and stimulant effects and are also derivatives of the classic hallucinogen mescaline. However, limited toxicity information on proscaline and...

DOI: 10.1007/s00204-025-04010-6 Full text Forensic toxicology Metabolomics Phenethylamine detection Biomarkers +4

Elucidating the Phase I metabolism of psilocin in vitro.

Archives of Toxicology March 1, 2025 Junqi Chen, Ziteng Wang, Ching Yee Yong et al. 3 citations

Psilocin is a well-studied controlled substance with potential psychotherapeutic applications. However, research gaps remain regarding its metabolism. Our objective was to elucidate a comprehensive Phase I metabolic profile of psilocin to support its forensic management and clinical development. We utilized human enzymes from various sources to characterize the Phase I metabolism of psilocin...

DOI: 10.1007/s00204-024-03952-7 Full text Psilocin Psilocybin Metabolic pathways Biotransformation +6

The entactogen 3,4-methylenedioxymethamphetamine (MDMA; ecstasy) as a treatment aid in psychotherapy and its safety concerns.

Archives of Toxicology August 1, 2024 Brian A Baldo 5 citations

The phenylethylamine, 3,4-methylenedioxymethamphetamine (MDMA, 'ecstasy'), is the prototypical example of an entactogen. Its original placement in highly restrictive drug usage categories in the US and UK, led to an inevitable restriction on MDMA neuroscience research and treatment. The dominant pharmacological effects of MDMA are its properties of release and inhibition of reuptake of amine...

DOI: 10.1007/s00204-024-03765-8 Full text 3,4-methylenedioxymethamphetamine Ecstasy MDMA MDMA And PTSD MDMA Deaths +6

Off-target activity of NBOMes and NBOMe analogs at the µ opioid receptor.

Archives of Toxicology May 1, 2023 Marie H Deventer, Mattias Persson, Antonio Laus et al. 7 citations

New psychoactive substances (NPS) are introduced on the illicit drug market at a rapid pace. Their molecular targets are often inadequately elucidated, which contributes to the delayed characterization of their pharmacological effects. Inspired by earlier findings, this study set out to investigate the µ opioid receptor (MOR) activation potential of a large set of psychedelics, substances which...

DOI: 10.1007/s00204-023-03465-9 Full text Bioassay Molecular docking Nbome Off-target +2

Linking in vitro and ex vivo CB1 activity with serum concentrations and clinical features in 5F-MDMB-PICA users to better understand SCRAs and their metabolites.

Archives of Toxicology November 1, 2022 Liesl K Janssens, Simon Hudson, David M Wood et al.

Synthetic cannabinoid receptor agonists (SCRAs) pose a danger to public health. This study focused on individuals experiencing recreational drug toxicity who had used 5F-MDMB-PICA.Patient records were evaluated regarding vital signs, Glasgow Coma Scale (GCS) and clinical features. Liquid chromatography coupled to high-resolution mass spectrometry (LC-HRMS) confirmed and quantified the presence...

DOI: 10.1007/s00204-022-03355-6 Full text Activity-based Bioassay Characterization Clinical toxicology +2

New designer phenethylamines 2C-C and 2C-P have abuse potential and induce neurotoxicity in rodents.

Archives of Toxicology April 1, 2021 Young-Jung Kim, Shi-Xun Ma, Kwang-Hyun Hur et al. 10 citations

2C (2C-x) is the general name for the family of phenethylamines containing two methoxy groups at the 2 and 5 positions of the benzene ring. The abuse of 2C family drugs has grown rapidly, although the abuse potential and neurotoxic properties of 2C drugs have not yet been fully investigated. In this study, we investigated the abuse potential and neurotoxicity of...

DOI: 10.1007/s00204-021-02980-x Full text 2c-c 2c-p Neurotoxicity Designer drugs +18

Correction to: In vitro structure-activity relationship determination of 30 psychedelic new psychoactive substances by means of β-arrestin 2 recruitment to the serotonin 2A receptor.

Archives of Toxicology October 1, 2020 Eline Pottie, Annelies Cannaert, Christophe P Stove correction

It has been brought to the authors' attention that Fig. 1 of "In vitro structure-activity relationship determination of 30 psychedelic new psychoactive substances by means of β-arrestin 2 recruitment to the serotonin 2A receptor" contained a mistake in the structures for 2C-B-FLY and Bromo-DragonFLY. This has now been corrected. The authors apologize for any inconvenience caused.

DOI: 10.1007/s00204-020-02863-7 Full text Psychedelic research Psychedelics Psychedelic compounds New research +18

In vitro structure–activity relationship determination of 30 psychedelic new psychoactive substances by means of β-arrestin 2 recruitment to the serotonin 2A receptor

Archives of Toxicology July 5, 2020 Eline Pottie, Annelies Cannaert, Christophe P Stove 36 citations

Serotonergic psychedelics, substances exerting their effects primarily through the serotonin 2A receptor (5-HT2AR), continue to comprise a substantial portion of reported new psychoactive substances (NPS). The exact mechanisms of action of psychedelics still remain to be elucidated further, and certain pathways remain largely unexplored on a molecular level for this group of compounds. A...

DOI: 10.1007/s00204-020-02836-w Serotonergic Serotonin In vitro Bioassay +5

Designer drugs: mechanism of action and adverse effects

Archives of Toxicology April 1, 2020 Dino Luethi, Matthias E. Liechti 258 citations

Abstract Psychoactive substances with chemical structures or pharmacological profiles that are similar to traditional drugs of abuse continue to emerge on the recreational drug market. Internet vendors may at least temporarily sell these so-called designer drugs without adhering to legal statutes or facing legal consequences. Overall, the mechanism of action and adverse effects of designer...

DOI: 10.1007/s00204-020-02693-7 Full text Pharmacology Designer drug Mechanism of action Adverse effect +6

The hallucinogenic world of tryptamines: an updated review.

Archives of Toxicology August 1, 2015 Ana Margarida Araújo, Félix Carvalho, Maria de Lourdes Bastos et al. 290 citations

In the area of psychotropic drugs, tryptamines are known to be a broad class of classical or serotonergic hallucinogens. These drugs are capable of producing profound changes in sensory perception, mood and thought in humans and act primarily as agonists of the 5-HT2A receptor. Well-known tryptamines such as psilocybin contained in Aztec sacred mushrooms and N,N-dimethyltryptamine (DMT),...

DOI: 10.1007/s00204-015-1513-x Full text

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