Identification of a high-affinity binding site for dinotefuran in the nerve cord of the American cockroach

Authors: Miyagi, Satoshi; Komaki, Iori; Ozoe, Yoshihisa

Source: Pest Management Science, Volume 62, Number 4, April 2006 , pp. 293-298(6)

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Abstract:

The binding of the neonicotinoid insecticide dinotefuran to insect nicotinic acetylcholine receptors (nAChRs) was examined by a centrifugation method using the nerve cord membranes of American cockroaches and [³H]dinotefuran (78 Ci mmol⁻¹). The K_d and B_max values of [³H]dinotefuran binding were estimated to be 13.7 nM and 14.8 fmol 40 µg⁻¹ protein respectively by Scatchard analysis. Epibatidine, an nAChR agonist, showed a rather lower affinity to the dinotefuran binding site (IC₅₀ = 991 nM) than dinotefuran (IC₅₀ = 5.02 nM). Imidacloprid and nereistoxin displayed lower potencies than dinotefuran but higher potencies than epibatidine. The potencies of five dinotefuran analogues in inhibiting the specific binding of [³H]dinotefuran to nerve cord membranes were determined. A good correlation (r² = 0.970) was observed between the −log IC₅₀ values of the tested compounds and their piperonyl butoxide-synergised insecticidal activities (−log LD₅₀ values) against German cockroaches. The results indicate that a high-affinity binding site for dinotefuran is present in the nerve cord of the American cockroach and that the binding of ligands to the site leads to the manifestation of insecticidal activity. Copyright © 2006 Society of Chemical Industry

Keywords: binding site; cockroach; dinotefuran; neonicotinoids; nicotinic acetylcholine receptors

Document Type: Research article

DOI: http://dx.doi.org/10.1002/ps.1156

Publication date: 2006-04-01

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Identification of a high-affinity binding site for dinotefuran in the nerve cord of the American cockroach

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