ArticleBritish journal of pharmacology2015
Pharmacological profile of novel psychoactive benzofurans.
Article in British journal of pharmacology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 37 papers, 1 of them a synthesis that pooled it.
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Who cites it
37 citing papers in PubMed, 1 synthesis or guideline pooled it, 115 citations in OpenAlex.
- Pharmacotherapy of Patients Taking New Psychoactive Substances: A Systematic Review and Analysis of Case Reports.Frontiers in psychiatry · 2021Pooled it
- Acute effects of MDMA, MDA, lysine-MDMA, and lysine-MDA in a randomized, double-blind, placebo-controlled, crossover trial in healthy participants.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2026Trial
- Effects of psychostimulants on locomotor activity in the BTBR TPsychopharmacology · 2026Article
- Stereoselective, sex-dependent 5-HTNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2026Article
- Next-Generation MDMA Analogue SDMA: Pharmacological and Metabolic Insights.ACS chemical neuroscience · 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
- Emerging Illicit Drug "2C": A Case Report on Its Hallucinogenic and Stimulant Properties.Cureus · 2024Article
- The entactogen 3,4-methylenedioxymethamphetamine (MDMA; ecstasy) as a treatment aid in psychotherapy and its safety concerns.Archives of toxicology · 2024Review
- Locomotor and discriminative stimulus effects of three benzofuran compounds in comparison to abused psychostimulants.Drug and alcohol dependence reports · 2023Article
- Pharmacological affinity fingerprints derived from bioactivity data for the identification of designer drugs.Journal of cheminformatics · 2022Article
- Effects of a psychedelic 5-HT2A receptor agonist on anxiety-related behavior and fear processing in mice.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2022Article
- Filter Feature Selection for Unsupervised Clustering of Designer Drugs Using DFT Simulated IR Spectra Data.ACS omega · 2021Article
- Characterization of in vitro phase I metabolites of methamnetamine in human liver microsomes by liquid chromatography-quadrupole time-of-flight mass spectrometry.International journal of legal medicine · 2021Article
- Molecular Mechanisms of Action of Novel Psychoactive Substances (NPS). A New Threat for Young Drug Users with Forensic-Toxicological Implications.Life (Basel, Switzerland) · 2021Review
- Beyond ecstasy: Alternative entactogens to 3,4-methylenedioxymethamphetamine with potential applications in psychotherapy.Journal of psychopharmacology (Oxford, England) · 2021Review
- International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function.Pharmacological reviews · 2021Review
- The psychoactive aminoalkylbenzofuran derivatives, 5-APB and 6-APB, mimic the effects of 3,4-methylenedioxyamphetamine (MDA) on monoamine transmission in male rats.Psychopharmacology · 2020Article
- Syntheses and analytical characterizations of novel (2-aminopropyl)benzo[b]thiophene (APBT) based stimulants.Drug testing and analysis · 2020Article
- Synthesis of 3-selanylbenzo[RSC advances · 2020Article
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeBenzofurans are newly used psychoactive substances, but their pharmacology is unknown. The aim of the present study was to pharmacologically characterize benzofurans in vitro. EXPERIMENTAL APPROACH: We assessed the effects of the benzofurans 5-APB, 5-APDB, 6-APB, 6-APDB, 4-APB, 7-APB, 5-EAPB and 5-MAPDB and benzodifuran 2C-B-FLY on the human noradrenaline (NA), dopamine and 5-HT uptake transporters using HEK 293 cells that express the respective transporters. We also investigated the release of NA, dopamine and 5-HT from monoamine-preloaded cells, monoamine receptor-binding affinity and 5-HT2A and 5-HT2B receptor activation. KEY
resultsAll of the benzofurans inhibited NA and 5-HT uptake more than dopamine uptake, similar to methylenedioxymethamphetamine (MDMA) and unlike methamphetamine. All of the benzofurans also released monoamines and interacted with trace amine-associated receptor 1 (TA1 receptor), similar to classic amphetamines. Most benzofurans were partial 5-HT2A receptor agonists similar to MDMA, but also 5-HT2B receptor agonists, unlike MDMA and methamphetamine. The benzodifuran 2C-B-FLY very potently interacted with 5-HT2 receptors and also bound to TA1 receptors. CONCLUSIONS AND IMPLICATIONS: Despite very similar structures, differences were found in the pharmacological profiles of different benzofurans and compared with their amphetamine analogues. Benzofurans acted as indirect monoamine agonists that interact with transporters similarly to MDMA. The benzofurans also interacted with 5-HT receptors. This pharmacological profile probably results in MDMA-like entactogenic psychoactive properties. However, benzofurans induce 5-HT2B receptor activation associated with heart valve fibrosis. The pharmacology of 2C-B-FLY indicates predominant hallucinogenic properties and a risk for vasoconstriction.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.