ArticlePsychopharmacology2023
Plasma pharmacokinetics and pharmacodynamic effects of the 2-benzylbenzimidazole synthetic opioid, isotonitazene, in male rats.
Article in Psychopharmacology, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 31 citations in OpenAlex.
- Preclinical pharmacology of N-pyrrolidino "nitazene" opioids appearing in nonmedical drug markets.The Journal of pharmacology and experimental therapeutics · 2026Article
- 5-Methyl etodesnitazene human metabolism: LC-ESIAnalytical and bioanalytical chemistry · 2026Article
- Pharmacodynamic effects and plasma pharmacokinetics of N, N-dimethyltryptamine after intranasal versus subcutaneous administration in male rats.Psychopharmacology · 2026Article
- Clinical and toxicological epidemiology of intoxications by new psychoactive substances in Reunion Island.International journal of emergency medicine · 2025Article
- The emergence of nitazenes: a new chapter in the synthetic opioid crisis.Archives of toxicology · 2025Review
- Pharmacology of newly identified nitazene variants reveals structural determinants of affinity, potency, selectivity for mu opioid receptors.Neuropharmacology · 2025Article
- Latest developments in small molecule analgesics: heterocyclic scaffolds I.Future medicinal chemistry · 2025Review
- Response to "Comment on Naloxone Dosing and Hospitalization for Nitazene Overdose: A Scoping Review".Journal of medical toxicology : official journal of the American College of Medical Toxicology · 2025Article
- Comment on "Naloxone Dosing and Hospitalization for Nitazene Overdose: A Scoping Review".Journal of medical toxicology : official journal of the American College of Medical Toxicology · 2025Article
- Characterization of novel nitazene recreational drugs: Insights into their risk potential from in vitro µ-opioid receptor assays and in vivo behavioral studies in mice.Pharmacological research · 2024Article
- Evaluation of Short-Term Stability of Different Nitazenes Psychoactive Opioids in Dried Blood Spots by Liquid Chromatography-High-Resolution Mass Spectrometry.International journal of molecular sciences · 2024Article
- In vitro structure-activity relationships and forensic case series of emerging 2-benzylbenzimidazole 'nitazene' opioids.Archives of toxicology · 2024Article
- Pharmacologic Characterization of Substituted Nitazenes atThe Journal of pharmacology and experimental therapeutics · 2024Article
- In Vitro Functional Profiling of Fentanyl and Nitazene Analogs at the μ-Opioid Receptor Reveals High Efficacy for Gi Protein Signaling.ACS chemical neuroscience · 2024Article
- Metabolic characterization of the new benzimidazole synthetic opioids - nitazenes.Frontiers in pharmacology · 2024Article
- Alkoxy chain length governs the potency of 2-benzylbenzimidazole 'nitazene' opioids associated with human overdose.Psychopharmacology · 2023Article
- Comparative neuropharmacology of structurally distinct non-fentanyl opioids that are appearing on recreational drug markets worldwide.Drug and alcohol dependence · 2023Article
- Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
rationaleIsotonitazene is an illicit synthetic opioid associated with many intoxications and fatalities. Recent studies show that isotonitazene is a potent µ-opioid receptor (MOR) agonist in vitro, but little information is available about its in vivo effects.
objectivesThe aims of the present study were to investigate the pharmacokinetics of isotonitazene in rats, and relate pharmacokinetic parameters to pharmacodynamic effects.
methodsIsotonitazene and its metabolites were identified and quantified by liquid chromatography tandem quadrupole mass spectrometry (LC-QQQ-MS). Male Sprague-Dawley rats with jugular catheters and subcutaneous (s.c.) temperature transponders received isotonitazene (3, 10, 30 µg/kg, s.c.) or its vehicle. Blood samples were drawn at 15, 30, 60, 120, and 240 min post-injection, and plasma was assayed using LC-QQQ-MS. At each blood draw, body temperature, catalepsy scores, and hot plate latencies were recorded.
resultsMaximum plasma concentrations of isotonitazene rose in parallel with increasing dose (range 0.2-9.8 ng/mL) and half-life ranged from 23.4 to 63.3 min. The metabolites 4'-hydroxy nitazene and N-desethyl isotonitazene were detected, and plasma concentrations were below the limit of quantitation (0.5 ng/mL) but above the limit of detection (0.1 ng/mL). Isotonitazene produced antinociception (ED
conclusionsIn summary, isotonitazene is a potent MOR agonist whose pharmacodynamic effects are related to circulating concentrations of the parent drug. The high potency of isotonitazene portends substantial risk to users who are exposed to the drug.
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