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J Agric Food Chem ; 65(36): 7865-7873, 2017 Sep 13.
Artigo em Inglês | MEDLINE | ID: mdl-28820587

RESUMO

A novel chemotype insecticide flupyrimin (FLP) [N-[(E)-1-(6-chloro-3-pyridinylmethyl)pyridin-2(1H)-ylidene]-2,2,2-trifluoroacetamide], discovered by Meiji Seika Pharma, has unique biological properties, including outstanding potency to imidacloprid (IMI)-resistant rice pests together with superior safety toward pollinators. Intriguingly, FLP acts as a nicotinic antagonist in American cockroach neurons, and [3H]FLP binds to the multiple high-affinity binding components in house fly nicotinic acetylcholine (ACh) receptor (nAChR) preparation. One of the [3H]FLP receptors is identical to the IMI receptor, and the alternative is IMI-insensitive subtype. Furthermore, FLP is favorably safe to rats as predicted by the very low affinity to the rat α4ß2 nAChR. Structure-activity relationships of FLP analogues in terms of receptor potency, featuring the pyridinylidene and trifluoroacetyl pharmacophores, were examined, thereby establishing the FLP molecular recognition at the Aplysia californica ACh-binding protein, a suitable structural surrogate of the insect nAChR. These FLP pharmacophores account for the excellent receptor affinity, accordingly revealing differences in its binding mechanism from IMI.


Assuntos
Inseticidas/química , Inseticidas/farmacologia , Antagonistas Nicotínicos/química , Antagonistas Nicotínicos/farmacologia , Receptores Nicotínicos/química , Animais , Aplysia/efeitos dos fármacos , Aplysia/metabolismo , Sítios de Ligação , Proteínas de Insetos/química , Proteínas de Insetos/metabolismo , Cinética , Periplaneta/efeitos dos fármacos , Periplaneta/genética , Periplaneta/metabolismo , Ratos , Receptores Nicotínicos/metabolismo , Relação Estrutura-Atividade
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