publication . Article . 2017

The novel isoxazoline ectoparasiticide lotilaner (Credelio™): a non-competitive antagonist specific to invertebrates γ-aminobutyric acid-gated chloride channels (GABACls)

Rufener, Lucien; Danelli, Vanessa; Bertrand, Daniel; Sager, Heinz;
Open Access English
  • Published: 01 Nov 2017 Journal: Parasites & Vectors, volume 10 (issn: 1756-3305, eissn: 1756-3305, Copyright policy)
  • Publisher: BMC
Abstract
Background The 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. Methods In 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), Lepeophtheir...
Subjects
free text keywords: RC109-216, Infectious and parasitic diseases, Isoxazoline, Non-competitive antagonist, GABACl, Invertebrates, Research, Lotilaner, γ-aminobutyric acid-gated chloride channels
38 references, page 1 of 3

Raymond, V, Sattelle, DB. Novel animal-health drug targets from ligand-gated chloride channels. Nat Rev Drug Discov. 2002; 1: 427-436 [PubMed] [DOI]

Ozoe, Y, Takeda, M, Kazuhiko, M. γ-Aminobutyric acid receptors: a rationale for developing selective insect pest control chemicals. In: Ishaaya IHAR, editor. Biorational control of arthropod pests: application and resistance management. 2009: 131-162

Lawrence, LJ, Casida, JE. Interactions of lindane, toxaphene and cyclodienes with brain-specific t-butylbicyclophosphorothionate receptor. Life Sci. 1984; 35: 171-178 [PubMed] [DOI]

Ghiasuddin, SM, Matsumura, F. Inhibition of gamma-aminobutyric acid (GABA)-induced chloride uptake by gamma-BHC and heptachlor epoxide. Comp Biochem Physiol C Comp Pharmacol. 1982; 73: 141-144 [DOI]

Sparks, TC, Dripps, JE, Watson, GB, Paroonagian, D. Resistance and cross-resistance to the spinosyns - a review and analysis. Pestic Biochem Physiol. 2012; 102: 1-10 [DOI]

Tingle, CCD, Rother, JA, Dewhurst, CF, Lauer, S, King, WJ. Fipronil: environmental fate, ecotoxicology, and human health concerns. Rev Environ Contam Toxicol. 2003; 176: 1-66 [PubMed]

Ffrench-Constant, RH, Rocheleau, TA, Steichen, JC, Chalmers, AE. A point mutation in a Drosophila GABA receptor confers insecticide resistance. Nature. 1993; 363: 449-451 [PubMed] [DOI]

Buckingham, SD, Biggin, PC, Sattelle, BM, Brown, LA, Sattelle, DB. Insect GABA receptors: splicing, editing, and targeting by antiparasitics and insecticides. Mol Pharmacol. 2005; 68: 942-951 [PubMed] [DOI]

Hosie, AM, Baylis, HA, Buckingham, SD, Sattelle, DB. Actions of the insecticide fipronil, on dieldrin-sensitive and- resistant GABA receptors of Drosophila Melanogaster. Br J Pharmacol. 1995; 115: 909-912 [OpenAIRE] [PubMed] [DOI]

Nakao, T, Hama, M, Kawahara, N, Hirase, K. Fipronil resistance in Sogatella furcifera: molecular cloning and functional expression of wild-type and mutant RDL GABA receptor subunits. J Pest Sci. 2012; 37: 37-44 [DOI]

Le Goff, G, Hamon, A, Bergé, J-B, Amichot, M. Resistance to fipronil in Drosophila simulans: influence of two point mutations in the RDL GABA receptor subunit. J Neurochem. 2005; 92: 1295-1305 [PubMed] [DOI]

Shoop, WL, Hartline, EJ, Gould, BR, Waddell, ME, McDowell, RG, Kinney, JB. Discovery and mode of action of afoxolaner, a new isoxazoline parasiticide for dogs. Vet Parasitol. 2014; 201: 179-189 [OpenAIRE] [PubMed] [DOI]

Curtis, MP, Vaillancourt, V, Goodwin, RM, Chubb, NAL, Howson, W, McTier, TL. Design and synthesis of sarolaner, a novel, once-a-month, oral isoxazoline for the control of fleas and ticks on dogs. Bioorg Med Chem Lett. 2016; 26: 1831-1835 [PubMed] [DOI]

Asahi, M, Kobayashi, M, Matsui, H, Nakahira, K. Differential mechanisms of action of the novel γ-aminobutyric acid receptor antagonist ectoparasiticides fluralaner (A1443) and fipronil. Pest Manag Sci. 2015; 71: 91-95 [PubMed] [DOI]

Zhao, C, Casida, JE. Insect γ-aminobutyric acid receptors and isoxazoline insecticides: toxicological profiles relative to the binding sites of [3H]fluralaner, [3H]-4′-ethynyl-4-n-propylbicycloorthobenzoate, and [3H]avermectin. J Agric Food Chem. 2014; 62: 1019-1024 [PubMed] [DOI]

38 references, page 1 of 3
Abstract
Background The 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. Methods In 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), Lepeophtheir...
Subjects
free text keywords: RC109-216, Infectious and parasitic diseases, Isoxazoline, Non-competitive antagonist, GABACl, Invertebrates, Research, Lotilaner, γ-aminobutyric acid-gated chloride channels
38 references, page 1 of 3

Raymond, V, Sattelle, DB. Novel animal-health drug targets from ligand-gated chloride channels. Nat Rev Drug Discov. 2002; 1: 427-436 [PubMed] [DOI]

Ozoe, Y, Takeda, M, Kazuhiko, M. γ-Aminobutyric acid receptors: a rationale for developing selective insect pest control chemicals. In: Ishaaya IHAR, editor. Biorational control of arthropod pests: application and resistance management. 2009: 131-162

Lawrence, LJ, Casida, JE. Interactions of lindane, toxaphene and cyclodienes with brain-specific t-butylbicyclophosphorothionate receptor. Life Sci. 1984; 35: 171-178 [PubMed] [DOI]

Ghiasuddin, SM, Matsumura, F. Inhibition of gamma-aminobutyric acid (GABA)-induced chloride uptake by gamma-BHC and heptachlor epoxide. Comp Biochem Physiol C Comp Pharmacol. 1982; 73: 141-144 [DOI]

Sparks, TC, Dripps, JE, Watson, GB, Paroonagian, D. Resistance and cross-resistance to the spinosyns - a review and analysis. Pestic Biochem Physiol. 2012; 102: 1-10 [DOI]

Tingle, CCD, Rother, JA, Dewhurst, CF, Lauer, S, King, WJ. Fipronil: environmental fate, ecotoxicology, and human health concerns. Rev Environ Contam Toxicol. 2003; 176: 1-66 [PubMed]

Ffrench-Constant, RH, Rocheleau, TA, Steichen, JC, Chalmers, AE. A point mutation in a Drosophila GABA receptor confers insecticide resistance. Nature. 1993; 363: 449-451 [PubMed] [DOI]

Buckingham, SD, Biggin, PC, Sattelle, BM, Brown, LA, Sattelle, DB. Insect GABA receptors: splicing, editing, and targeting by antiparasitics and insecticides. Mol Pharmacol. 2005; 68: 942-951 [PubMed] [DOI]

Hosie, AM, Baylis, HA, Buckingham, SD, Sattelle, DB. Actions of the insecticide fipronil, on dieldrin-sensitive and- resistant GABA receptors of Drosophila Melanogaster. Br J Pharmacol. 1995; 115: 909-912 [OpenAIRE] [PubMed] [DOI]

Nakao, T, Hama, M, Kawahara, N, Hirase, K. Fipronil resistance in Sogatella furcifera: molecular cloning and functional expression of wild-type and mutant RDL GABA receptor subunits. J Pest Sci. 2012; 37: 37-44 [DOI]

Le Goff, G, Hamon, A, Bergé, J-B, Amichot, M. Resistance to fipronil in Drosophila simulans: influence of two point mutations in the RDL GABA receptor subunit. J Neurochem. 2005; 92: 1295-1305 [PubMed] [DOI]

Shoop, WL, Hartline, EJ, Gould, BR, Waddell, ME, McDowell, RG, Kinney, JB. Discovery and mode of action of afoxolaner, a new isoxazoline parasiticide for dogs. Vet Parasitol. 2014; 201: 179-189 [OpenAIRE] [PubMed] [DOI]

Curtis, MP, Vaillancourt, V, Goodwin, RM, Chubb, NAL, Howson, W, McTier, TL. Design and synthesis of sarolaner, a novel, once-a-month, oral isoxazoline for the control of fleas and ticks on dogs. Bioorg Med Chem Lett. 2016; 26: 1831-1835 [PubMed] [DOI]

Asahi, M, Kobayashi, M, Matsui, H, Nakahira, K. Differential mechanisms of action of the novel γ-aminobutyric acid receptor antagonist ectoparasiticides fluralaner (A1443) and fipronil. Pest Manag Sci. 2015; 71: 91-95 [PubMed] [DOI]

Zhao, C, Casida, JE. Insect γ-aminobutyric acid receptors and isoxazoline insecticides: toxicological profiles relative to the binding sites of [3H]fluralaner, [3H]-4′-ethynyl-4-n-propylbicycloorthobenzoate, and [3H]avermectin. J Agric Food Chem. 2014; 62: 1019-1024 [PubMed] [DOI]

38 references, page 1 of 3
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publication . Article . 2017

The novel isoxazoline ectoparasiticide lotilaner (Credelio™): a non-competitive antagonist specific to invertebrates γ-aminobutyric acid-gated chloride channels (GABACls)

Rufener, Lucien; Danelli, Vanessa; Bertrand, Daniel; Sager, Heinz;