ArticlePsychopharmacology2020
The psychoactive aminoalkylbenzofuran derivatives, 5-APB and 6-APB, mimic the effects of 3,4-methylenedioxyamphetamine (MDA) on monoamine transmission in male rats.
Article in Psychopharmacology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers, 1 of them a synthesis that pooled it.
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Who cites it
9 citing papers in PubMed, 1 synthesis or guideline pooled it, 18 citations in OpenAlex.
- Pharmacotherapy of Patients Taking New Psychoactive Substances: A Systematic Review and Analysis of Case Reports.Frontiers in psychiatry · 2021Pooled it
- Neuropharmacology of levamisole and its phase I metabolites: lack of evidence for levamisole-cocaine interactions.Psychopharmacology · 2026Article
- Dose-effect analysis of 6-APB ("Benzofury") on fear memory, motor behavior, and reward.Psychopharmacology · 2026Article
- Prolintane analogs as hybrid monoamine transporter ligands: Structural determinants and species differences.The Journal of biological chemistry · 2025Article
- New psychoactive substances: a multidisciplinary review of challenges and their diverse character.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2025Review
- Novel Benzofuran Derivatives Induce Monoamine Release and Substitute for the Discriminative Stimulus Effects of 3,4-Methylenedioxymethamphetamine.The Journal of pharmacology and experimental therapeutics · 2024Article
- Locomotor and discriminative stimulus effects of three benzofuran compounds in comparison to abused psychostimulants.Drug and alcohol dependence reports · 2023Article
- (2-Aminopropyl)benzo[β]thiophenes (APBTs) are novel monoamine transporter ligands that lack stimulant effects but display psychedelic-like activity in mice.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2022Article
- Domino C-C/C-O bond formation: palladium-catalyzed regioselective synthesis of 7-iodobenzo[RSC advances · 2021Article
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Authors and funding
6 authors at 4 institutions in 3 countries.
Funding
Abstract
rationaleThe nonmedical use of new psychoactive substances (NPS) is a worldwide public health concern. The so-called "benzofury" compounds, 5-(2-aminopropyl)benzofuran (5-APB) and 6-(2-aminopropyl)benzofuran (6-APB), are NPS with stimulant-like properties in human users. These substances are known to interact with monoamine transporters and 5-HT receptors in transfected cells, but less is known about their effects in animal models.
methodsHere, we used in vitro monoamine transporter assays in rat brain synaptosomes to characterize the effects of 5-APB and 6-APB, together with their N-methyl derivatives 5-MAPB and 6-MAPB, in comparison with 3,4-methylenedioxyamphetamine (MDA) and 3,4-methylenedioxymethamphetamine (MDMA). In vivo neurochemical and behavioral effects of 5-APB (0.3 and 1.0 mg/kg, i.v.) and 6-APB (0.3 and 1.0 mg/kg, i.v.) were assessed in comparison with MDA (1.0 and 3.0 mg/kg, i.v.) using microdialysis sampling in the nucleus accumbens of conscious male rats.
resultsAll four benzofuran derivatives were substrate-type releasers at dopamine transporters (DAT), norepinephrine transporters (NET), and serotonin transporters (SERT) with nanomolar potencies, similar to the profile of effects produced by MDA and MDMA. However, the benzofurans were at least threefold more potent than MDA and MDMA at evoking transporter-mediated release. Like MDA, both benzofurans induced dose-related elevations in extracellular dopamine and serotonin in the brain, but benzofurans were more potent than MDA. The benzofuran derivatives also induced profound behavioral activation characterized by forward locomotion which lasted for at least 2 h post-injection.
conclusionsOverall, benzofurans are more potent than MDA in vitro and in vivo, producing sustained stimulant-like effects in rats. These data suggest that benzofuran-type compounds may have abuse liability and could pose risks for adverse effects, especially if used in conjunction with abused drugs or medications which enhance monoamine transmission in the brain.
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