ArticleBritish journal of pharmacology2012
Mechanism of action of the insecticides, lindane and fipronil, on glycine receptor chloride channels.
Article in British journal of pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 89 citations in OpenAlex.
- New hyperekplexia mutations provide insight into glycine receptor assembly, trafficking, and activation mechanisms.The Journal of biological chemistry · 2013Trial
- Metal-Free Oxidative Functionalization of Allylic Sulfones/Allylic Triflones with Water Participation Enabled by Hypervalent Iodine Reagents.Molecules (Basel, Switzerland) · 2026Article
- Bis(trifluoromethyl)disulfide and the EtPChemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- Designing Trifluoromethyl Pyrazolones for Selective Molluscicidal Activity AgainstJournal of agricultural and food chemistry · 2025Article
- Modeling the developing nervous system: a neuroscience perspective on the use of new approach methodologies in developmental neurotoxicity testing.Toxicological sciences : an official journal of the Society of Toxicology · 2025Review
- Electrically silent mutants unravel the mechanism of binding-gating coupling in Cys-loop receptors.Science advances · 2024Article
- Can the increase in atmospheric temperature enhance the toxicity and risk of fipronil for collembolans in tropical soils?Environmental science and pollution research international · 2022Article
- Building a Network of Adverse Outcome Pathways (AOPs) Incorporating the Tau-Driven AOP Toward Memory Loss (AOP429).Journal of Alzheimer's disease reports · 2022Review
- Genome-Wide Selective Signature Analysis Revealed Insecticide Resistance Mechanisms inInsects · 2021Article
- Vitamin C Attenuates Oxidative Stress and Behavioral Abnormalities Triggered by Fipronil and Pyriproxyfen Insecticide Chronic Exposure on Zebrafish Juvenile.Antioxidants (Basel, Switzerland) · 2020Article
- The effects of insecticides on two splice variants of the glutamate-gated chloride channel receptor of the major malaria vector, Anopheles gambiae.British journal of pharmacology · 2020Article
- Evaluation of the sensitivity spectrum of a video tracking system with zebrafish (Danio rerio) exposed to five different toxicants.Environmental science and pollution research international · 2017Article
- Voltage-Dependent Inhibition of Glycine Receptor Channels by Niflumic Acid.Frontiers in molecular neuroscience · 2017Article
- A Recombinant Human Pluripotent Stem Cell Line Stably Expressing Halide-Sensitive YFP-I152L for GABAAR and GlyR-Targeted High-Throughput Drug Screening and Toxicity Testing.Frontiers in molecular neuroscience · 2016Article
- Selective potentiation of alpha 1 glycine receptors by ginkgolic acid.Frontiers in molecular neuroscience · 2015Article
- An atypical residue in the pore of Varroa destructor GABA-activated RDL receptors affects picrotoxin block and thymol modulation.Insect biochemistry and molecular biology · 2014Article
- Novel missense mutations in the glycine receptor β subunit gene (GLRB) in startle disease.Neurobiology of disease · 2013Article
- Fluorescence-based high-throughput functional profiling of ligand-gated ion channels at the level of single cells.PloS one · 2013Article
- The pharmacological profile of ELIC, a prokaryotic GABA-gated receptor.Neuropharmacology · 2012Article
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeDocking studies predict that the insecticides, lindane and fipronil, block GABA(A) receptors by binding to 6' pore-lining residues. However, this has never been tested at any Cys-loop receptor. The neurotoxic effects of these insecticides are also thought to be mediated by GABA(A) receptors, although a recent morphological study suggested glycine receptors mediated fipronil toxicity in zebrafish. Here we investigated whether human α1, α1β, α2 and α3 glycine receptors were sufficiently sensitive to block by either compound as to represent possible neurotoxicity targets. We also investigated the mechanisms by which lindane and fipronil inhibit α1 glycine receptors. EXPERIMENTAL APPROACH: Glycine receptors were recombinantly expressed in HEK293 cells and insecticide effects were studied using patch-clamp electrophysiology. KEY
resultsBoth compounds completely inhibited all tested glycine receptor subtypes with IC(50) values ranging from 0.2-2 µM, similar to their potencies at vertebrate GABA(A) receptors. Consistent with molecular docking predictions, both lindane and fipronil interacted with 6' threonine residues via hydrophobic interactions and hydrogen bonds. In contrast with predictions, we found no evidence for lindane interacting at the 2' level. We present evidence for fipronil binding in a non-blocking mode in the anaesthetic binding pocket, and for lindane as an excellent pharmacological tool for identifying the presence of β subunits in αβ heteromeric glycine receptors. CONCLUSIONS AND IMPLICATIONS: This study implicates glycine receptors as novel vertebrate toxicity targets for fipronil and lindane. Furthermore, lindane interacted with pore-lining 6' threonine residues, whereas fipronil may have both pore and non-pore binding sites.
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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.