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. 2015 Jan;71(1):91-5.
doi: 10.1002/ps.3768. Epub 2014 Mar 31.

Differential mechanisms of action of the novel γ-aminobutyric acid receptor antagonist ectoparasiticides fluralaner (A1443) and fipronil

Miho Asahi  1 , Masaki Kobayashi, Hiroto Matsui, Kunimitsu Nakahira
Affiliations

Differential mechanisms of action of the novel γ-aminobutyric acid receptor antagonist ectoparasiticides fluralaner (A1443) and fipronil

Miho Asahi et al. Pest Manag Sci. 2015 Jan.

Abstract

Background: Fluralaner (A1443) is an isoxazoline ectoparasiticide that is a novel antagonist of γ-aminobutyric acid (GABA) receptors (GABARs), with a potency comparable to that of fipronil, a phenylpyrazole ectoparasiticide. To clarify the biological effectiveness of fluralaner against fipronil-resistant pests, differences in the actions of fluralaner and fipronil on GABARs that possess resistance to dieldrin (rdl)-type mutations were evaluated.

Results: Fipronil had neither pest control nor GABAR-antagonistic activities against two-spotted spider mites (Tetranychus urticae) that had two different rdl-type amino acids (A(301) → H and T(350) → A: Drosophila melanogaster GABAR numbering) and against small brown planthoppers (Laodelphax striatellus) that had a novel rdl-type (A(283) → N) mutation in GABARs. In contrast, fluralaner showed not only high pest control activities against these pests, but also excellent antagonistic activities for these rdl-type GABARs.

Conclusion: The findings indicate that rdl-type fipronil-resistant pests do not show cross-resistance to fluralaner owing to the differential actions of fluralaner and fipronil on the GABAR.

Keywords: A1443; GABA; fluralaner; ligand-gated ion channel; parasiticide; receptor.

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