2016
DOI: 10.1002/ps.4412
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Amitraz and its metabolite differentially activate α‐ and β‐adrenergic‐like octopamine receptors

Abstract: Although both amitraz and DPMF acted as OAR agonists, the metabolite DPMF was more potent than amitraz and differentially activated α- and β-AL OARs. The present findings provide a basis for studies to examine the mechanism of amitraz resistance and to develop novel acaricides and insecticides. © 2016 Society of Chemical Industry.

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Cited by 62 publications
(47 citation statements)
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“…). It is believed that NlOARs play a critical role in the central nervous system and the high enrichment of these NlOARs within the central nervous system has been beneficial for the exploitation of insecticides targeting these receptors . In Malpighian tubules, an important tissue for urine production and ion exchange, NlOA1 was the most highly expressed gene compared with others.…”
Section: Resultsmentioning
confidence: 99%
“…). It is believed that NlOARs play a critical role in the central nervous system and the high enrichment of these NlOARs within the central nervous system has been beneficial for the exploitation of insecticides targeting these receptors . In Malpighian tubules, an important tissue for urine production and ion exchange, NlOA1 was the most highly expressed gene compared with others.…”
Section: Resultsmentioning
confidence: 99%
“…This provides a structural and functional basis for the development of specific insecticides. The β‐OAR is an important molecular target for formamidine insecticides (Kita et al., ). For example, amitraz is a formamidine acaricide insecticide used to control ticks, mites, and fleas.…”
Section: Discussionmentioning
confidence: 99%
“…At amitraz concentrations of 1, 10, and 100 μM, intracellular cAMP concentrations were 1.75, 6.35, and 20.5 times higher than in controls. Furthermore, both amitraz and its metabolite N2‐(2,4‐dimethylphenyl)‐N1‐methyformamidine (DPMF) acted as OAR agonists, and the metabolite DPMF was more potent than amitraz‐activated β‐adrenergic‐like OARs (Kita et al., ). We speculate that the weak affinity of amitraz for the β‐OAR might be one reason that amitraz could not be used to control Lepidoptera pests.…”
Section: Discussionmentioning
confidence: 99%
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“…Octopamine and tyramine receptors are types of Gprotein coupled receptors that increase intracellular Ca 2+ concentrations and/or activate molecular signaling cascades [54]. These receptors are the target sites for formamidine insecticides, such as amitraz that is used as a miticide to control Varroa mites in honey bee colonies [55,56]. Mutations in these receptors may underlie amitraz resistance [57,58].…”
Section: Introductionmentioning
confidence: 99%