ArticleParasites & vectors2017
The novel isoxazoline ectoparasiticide lotilaner (Credelio™): a non-competitive antagonist specific to invertebrates γ-aminobutyric acid-gated chloride channels (GABACls).
Article in Parasites & vectors, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 73 citations in OpenAlex.
- A randomized, controlled field study to assess the efficacy and safety of lotilaner (Credelio™) in controlling fleas in client-owned cats in Europe.Parasites & vectors · 2018Trial
- A randomized, controlled study to assess the efficacy and safety of lotilaner (Credelio™) in controlling ticks in client-owned dogs in Europe.Parasites & vectors · 2017Trial
- Pharmacokinetics, Absolute Bioavailability, and Nonlinear Topical Absorption of a Fluralaner-Moxidectin Spot-On Formulation in Cats.Veterinary sciences · 2026Article
- FDA-Approved Drugs Containing Amide Functionality in the Last Five Years (2021-2025): Pharmaceutical Use, Trends and Synthetic Approaches.Medicines (Basel, Switzerland) · 2026Review
- Efficacy of Credelio Quattro™ chewable tablets containing lotilaner, moxidectin, pyrantel, and praziquantel against Ctenocephalides felis and Rhipicephalus sanguineus infestations on dogs.Parasites & vectors · 2026Article
- Article
- First report of VGSC mutations for resistance to synthetic pyrethroids in brown dog ticks (Rhipicephalus sanguineus sensu stricto) from Brazil.Parasites & vectors · 2025Article
- Assessment of lotilaner (Credelio® CAT) for control of in-home Ctenocephalides felis infestations.Parasites & vectors · 2025Article
- The Structural Basis of Binding Stability and Selectivity of Sarolaner Enantiomers forMolecules (Basel, Switzerland) · 2025Article
- Comparative analysis of isoxazoline activity on human and canine GABA receptors expressed in Xenopus oocytes.Parasites & vectors · 2025Article
- Lotilaner Ophthalmic Solution, 0.25%, for the Treatment ofHealthcare (Basel, Switzerland) · 2024Review
- Highlights on Fluorine-containing Drugs Approved by U.S. FDA in 2023.Current topics in medicinal chemistry · 2024Review
- Emerging Medical Therapies in Rosacea: A Narrative Review.Dermatology and therapy · 2023Review
- G3'MTMD3 in the insect GABA receptor subunit, RDL, confers resistance to broflanilide and fluralaner.PLoS genetics · 2023Article
- Putative target sites in synganglion for novel ixodid tick control strategies.Ticks and tick-borne diseases · 2023Review
- Discovery of a Novel Class of Acylthiourea-Containing Isoxazoline Insecticides againstMolecules (Basel, Switzerland) · 2023Article
- Pharmacokinetic and pharmacodynamic considerations for treating sarcoptic mange with cross-relevance to Australian wildlife.International journal for parasitology. Drugs and drug resistance · 2023Review
- Efficacy of lotilaner against myiasis caused by Cochliomyia hominivorax (Diptera: Calliphoridae) in naturally infested dogs.Parasites & vectors · 2023Article
- Molecular targets for the development of new acaricides againstParasitology · 2022Review
- Transcriptome of the synganglion in the tick Ixodes ricinus and evolution of the cys-loop ligand-gated ion channel family in ticks.BMC genomics · 2022Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundThe isoxazolines are a novel class of parasiticides that are potent inhibitors of γ-aminobutyric acid (GABA)-gated chloride channels (GABACls) and, to a lesser extent, of inhibitory glutamate-gated chloride channels (GluCls). Lotilaner (Credelio™), a novel representative of this chemical class, is currently evaluated for its excellent ectoparasiticide properties.
methodsIn this study, we investigated the molecular mode of action and pharmacology of lotilaner. We report the successful gene identification, cDNA cloning and functional expression in Xenopus oocytes of Drosohpila melanogaster (wild type and dieldrin/fipronil-resistant forms), Lepeophtheirus salmonis (an ectoparasite copepod crustacean of salmon), Rhipicephalus microplus and Canis lupus familiaris GABACls. Automated Xenopus oocyte two-electrode voltage clamp electrophysiology was used to assess GABACls functionality and to compare ion channel inhibition by lotilaner with that of established insecticides addressing GABACls as targets.
resultsIn these assays, we demonstrated that lotilaner is a potent non-competitive antagonist of insects (fly) GABACls. No cross-resistance with dieldrin or fipronil resistance mutations was detected, suggesting that lotilaner might bind to a site at least partly different from the one bound by known GABACl blockers. Using co-application experiments, we observed that lotilaner antagonism differs significantly from the classical open channel blocker fipronil. We finally confirmed for the first time that isoxazoline compounds are not only powerful antagonists of GABACls of acari (ticks) but also of crustaceans (sea lice), while no activity on a dog GABA
conclusionsTogether, these results demonstrate that lotilaner is a non-competitive antagonist specific to invertebrate's γ-aminobutyric acid-gated chloride channels (GABACls). They contribute to our understanding of the mode of action of this new ectoparasiticide compound.
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