ArticleNeurochemistry international2014
Aminorex, a metabolite of the cocaine adulterant levamisole, exerts amphetamine like actions at monoamine transporters.
Article in Neurochemistry international, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
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Who cites it
35 citing papers in PubMed, 113 citations in OpenAlex.
- Neuropharmacology of levamisole and its phase I metabolites: lack of evidence for levamisole-cocaine interactions.Psychopharmacology · 2026Article
- Meta-analysis of levamisole absorption and disposition across diverse species using a minimal physiologically-based pharmacokinetic model.Journal of pharmaceutical investigation · 2026Article
- Utilizing Caenorhabditis Elegans as a Rapid and Precise Model for Assessing Amphetamine-Type Stimulants: A Novel Approach to Evaluating New Psychoactive Substances Activity and Mechanisms.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Health risks of cocaine adulteration: local anesthetics as modulators of monoamine and organic cation transporters.Frontiers in pharmacology · 2025Article
- Article
- Levamisole Impairs Vascular Function by Blocking α-Adrenergic Receptors and Reducing NO Bioavailability in Rabbit Renal Artery.Cardiovascular toxicology · 2024Article
- NETosis Secondary to the Use of Levamisole-Adulterated Cocaine: A Likely Underlying Mechanism of Vasculopathy.Journal of toxicology · 2024Article
- Development and validation of an automated microfluidic perfusion platform for parallelized screening of compounds in vitro.Basic & clinical pharmacology & toxicology · 2023Article
- [Cocaine-induced vasculitis and mimics of vasculitis].Zeitschrift fur Rheumatologie · 2023Review
- Applications and Potential of In Silico Approaches for Psychedelic Chemistry.Molecules (Basel, Switzerland) · 2023Review
- Levamisole-induced and COVID-19-induced retiform purpura: two overlapping, emerging clinical syndromes.Archives of dermatological research · 2023Review
- Synthesis and characterization of dDrug testing and analysis · 2023Article
- Characterization of Three Novel 4-Methylaminorex Derivatives Applied as Designer Drugs.Molecules (Basel, Switzerland) · 2022Article
- Double Suicide Due to the Ingestion of Levamisole-Adulterated Cocaine: Case Report and Review of the Literature.Academic forensic pathology · 2022Article
- Adverse reactions with levamisole vary according to its indications and misuse: A systematic pharmacovigilance study.British journal of clinical pharmacology · 2022Article
- Cocaine and Levamisole Induced Vasculitis.Cureus · 2021Article
- Use of levamisole-adulterated cocaine is associated with increased load of white matter lesions.Journal of psychiatry & neuroscience : JPN · 2021Article
- A fatal case after an intravenous injection of levamisole.Forensic science, medicine, and pathology · 2021Article
- An Overview of Cell-Based Assay Platforms for the Solute Carrier Family of Transporters.Frontiers in pharmacology · 2021Review
- The Amino Terminus of LeuT Changes Conformation in an Environment Sensitive Manner.Neurochemical research · 2020Article
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
Psychostimulants such as amphetamine and cocaine are illicitly used drugs that act on neurotransmitter transporters for dopamine, serotonin or norepinephrine. These drugs can by themselves already cause severe neurotoxicity. However, an additional health threat arises from adulterant substances which are added to the illicit compound without declaration. One of the most frequently added adulterants in street drugs sold as cocaine is the anthelmintic drug levamisole. We tested the effects of levamisole on neurotransmitter transporters heterologously expressed in HEK293 cells. Levamisole was 100 and 300-fold less potent than cocaine in blocking norepinephrine and dopamine uptake, and had only very low affinity for the serotonin transporter. In addition, levamisole did not trigger any appreciable substrate efflux. Because levamisole and cocaine are frequently co-administered, we searched for possible allosteric effects; at 30μM, a concentration at which levamisole displayed already mild effects on norepinephrine transport it did not enhance the inhibitory action of cocaine. Levamisole is metabolized to aminorex, a formerly marketed anorectic drug, which is classified as an amphetamine-like substance. We examined the uptake-inhibitory and efflux-eliciting properties of aminorex and found it to exert strong effects on all three neurotransmitter transporters in a manner similar to amphetamine. We therefore conclude that while the adulterant levamisole itself has only moderate effects on neurotransmitter transporters, its metabolite aminorex may exert distinct psychostimulant effects by itself. Given that the half-time of levamisole and aminorex exceeds that of cocaine, it may be safe to conclude that after the cocaine effect "fades out" the levamisole/aminorex effect "kicks in".
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Registered trials
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