Inhibition of Oryctolagus cuniculus (rabbit) AOX in liver cytosol at IC50 concentration
|
Oryctolagus cuniculus
|
8.0
%
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: oxidative stress in planta and metallo-oxidase inhibition.
Year : 2011
Volume : 59
Issue : 9
First Page : 4860
Last Page : 4867
Authors : Ford KA, Gulevich AG, Swenson TL, Casida JE.
Abstract : Neonicotinoids not only control insect pests but also sometimes independently alter plant growth and response to stress. We find that imidacloprid, thiacloprid, acetamiprid, thiamethoxam, and clothianidin but not nitenpyram and dinotefuran induce foliar lesions and peroxidative damage in soybean ( Glycine max ) seedlings assayed with the 3,3'-diaminobenzidine stain. The chloropyridinyl-carboxylic acid (COOH) but not the -carboxaldehyde (CHO) metabolites induce peroxidative damage but in a different pattern. Surprisingly, the chlorothiazolyl -CHO and -COOH metabolites induce chlorosis but no clear superimposable peroxidative damage or cell death. Four metallo-oxidases known to modulate reactive oxygen species were not sensitive in vitro to the parent neonicotinoid itself but were to several CHO and COOH metabolites and related compounds, with a sensitivity order of CHO > COOH and tyrosinase > xanthine oxidase and aldehyde oxidase > catalase. Although metallo-oxidase inhibition does not correlate overall with lesion formation, it may play an as yet unknown role in plant response to neonicotinoids.
Inhibition of xanthine oxidase at IC50 concentration
|
None
|
3.0
%
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: oxidative stress in planta and metallo-oxidase inhibition.
Year : 2011
Volume : 59
Issue : 9
First Page : 4860
Last Page : 4867
Authors : Ford KA, Gulevich AG, Swenson TL, Casida JE.
Abstract : Neonicotinoids not only control insect pests but also sometimes independently alter plant growth and response to stress. We find that imidacloprid, thiacloprid, acetamiprid, thiamethoxam, and clothianidin but not nitenpyram and dinotefuran induce foliar lesions and peroxidative damage in soybean ( Glycine max ) seedlings assayed with the 3,3'-diaminobenzidine stain. The chloropyridinyl-carboxylic acid (COOH) but not the -carboxaldehyde (CHO) metabolites induce peroxidative damage but in a different pattern. Surprisingly, the chlorothiazolyl -CHO and -COOH metabolites induce chlorosis but no clear superimposable peroxidative damage or cell death. Four metallo-oxidases known to modulate reactive oxygen species were not sensitive in vitro to the parent neonicotinoid itself but were to several CHO and COOH metabolites and related compounds, with a sensitivity order of CHO > COOH and tyrosinase > xanthine oxidase and aldehyde oxidase > catalase. Although metallo-oxidase inhibition does not correlate overall with lesion formation, it may play an as yet unknown role in plant response to neonicotinoids.
Inhibition of Agaricus bisporus (mushroom) tyrosinase at IC50 concentration
|
Agaricus bisporus
|
22.0
%
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: oxidative stress in planta and metallo-oxidase inhibition.
Year : 2011
Volume : 59
Issue : 9
First Page : 4860
Last Page : 4867
Authors : Ford KA, Gulevich AG, Swenson TL, Casida JE.
Abstract : Neonicotinoids not only control insect pests but also sometimes independently alter plant growth and response to stress. We find that imidacloprid, thiacloprid, acetamiprid, thiamethoxam, and clothianidin but not nitenpyram and dinotefuran induce foliar lesions and peroxidative damage in soybean ( Glycine max ) seedlings assayed with the 3,3'-diaminobenzidine stain. The chloropyridinyl-carboxylic acid (COOH) but not the -carboxaldehyde (CHO) metabolites induce peroxidative damage but in a different pattern. Surprisingly, the chlorothiazolyl -CHO and -COOH metabolites induce chlorosis but no clear superimposable peroxidative damage or cell death. Four metallo-oxidases known to modulate reactive oxygen species were not sensitive in vitro to the parent neonicotinoid itself but were to several CHO and COOH metabolites and related compounds, with a sensitivity order of CHO > COOH and tyrosinase > xanthine oxidase and aldehyde oxidase > catalase. Although metallo-oxidase inhibition does not correlate overall with lesion formation, it may play an as yet unknown role in plant response to neonicotinoids.
Inhibition of xanthine oxidase
|
None
|
1000000.0
nM
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: oxidative stress in planta and metallo-oxidase inhibition.
Year : 2011
Volume : 59
Issue : 9
First Page : 4860
Last Page : 4867
Authors : Ford KA, Gulevich AG, Swenson TL, Casida JE.
Abstract : Neonicotinoids not only control insect pests but also sometimes independently alter plant growth and response to stress. We find that imidacloprid, thiacloprid, acetamiprid, thiamethoxam, and clothianidin but not nitenpyram and dinotefuran induce foliar lesions and peroxidative damage in soybean ( Glycine max ) seedlings assayed with the 3,3'-diaminobenzidine stain. The chloropyridinyl-carboxylic acid (COOH) but not the -carboxaldehyde (CHO) metabolites induce peroxidative damage but in a different pattern. Surprisingly, the chlorothiazolyl -CHO and -COOH metabolites induce chlorosis but no clear superimposable peroxidative damage or cell death. Four metallo-oxidases known to modulate reactive oxygen species were not sensitive in vitro to the parent neonicotinoid itself but were to several CHO and COOH metabolites and related compounds, with a sensitivity order of CHO > COOH and tyrosinase > xanthine oxidase and aldehyde oxidase > catalase. Although metallo-oxidase inhibition does not correlate overall with lesion formation, it may play an as yet unknown role in plant response to neonicotinoids.
Inhibition of Oryctolagus cuniculus (rabbit) AOX in liver cytosol
|
Oryctolagus cuniculus
|
1000000.0
nM
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: oxidative stress in planta and metallo-oxidase inhibition.
Year : 2011
Volume : 59
Issue : 9
First Page : 4860
Last Page : 4867
Authors : Ford KA, Gulevich AG, Swenson TL, Casida JE.
Abstract : Neonicotinoids not only control insect pests but also sometimes independently alter plant growth and response to stress. We find that imidacloprid, thiacloprid, acetamiprid, thiamethoxam, and clothianidin but not nitenpyram and dinotefuran induce foliar lesions and peroxidative damage in soybean ( Glycine max ) seedlings assayed with the 3,3'-diaminobenzidine stain. The chloropyridinyl-carboxylic acid (COOH) but not the -carboxaldehyde (CHO) metabolites induce peroxidative damage but in a different pattern. Surprisingly, the chlorothiazolyl -CHO and -COOH metabolites induce chlorosis but no clear superimposable peroxidative damage or cell death. Four metallo-oxidases known to modulate reactive oxygen species were not sensitive in vitro to the parent neonicotinoid itself but were to several CHO and COOH metabolites and related compounds, with a sensitivity order of CHO > COOH and tyrosinase > xanthine oxidase and aldehyde oxidase > catalase. Although metallo-oxidase inhibition does not correlate overall with lesion formation, it may play an as yet unknown role in plant response to neonicotinoids.
Inhibition of Agaricus bisporus (mushroom) tyrosinase
|
Agaricus bisporus
|
1000000.0
nM
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: oxidative stress in planta and metallo-oxidase inhibition.
Year : 2011
Volume : 59
Issue : 9
First Page : 4860
Last Page : 4867
Authors : Ford KA, Gulevich AG, Swenson TL, Casida JE.
Abstract : Neonicotinoids not only control insect pests but also sometimes independently alter plant growth and response to stress. We find that imidacloprid, thiacloprid, acetamiprid, thiamethoxam, and clothianidin but not nitenpyram and dinotefuran induce foliar lesions and peroxidative damage in soybean ( Glycine max ) seedlings assayed with the 3,3'-diaminobenzidine stain. The chloropyridinyl-carboxylic acid (COOH) but not the -carboxaldehyde (CHO) metabolites induce peroxidative damage but in a different pattern. Surprisingly, the chlorothiazolyl -CHO and -COOH metabolites induce chlorosis but no clear superimposable peroxidative damage or cell death. Four metallo-oxidases known to modulate reactive oxygen species were not sensitive in vitro to the parent neonicotinoid itself but were to several CHO and COOH metabolites and related compounds, with a sensitivity order of CHO > COOH and tyrosinase > xanthine oxidase and aldehyde oxidase > catalase. Although metallo-oxidase inhibition does not correlate overall with lesion formation, it may play an as yet unknown role in plant response to neonicotinoids.
Phytotoxicity against Vitis vinifera seedlings assessed as lesions at 50 to 100 ppm after 9 days
|
Vitis vinifera
|
None
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: oxidative stress in planta and metallo-oxidase inhibition.
Year : 2011
Volume : 59
Issue : 9
First Page : 4860
Last Page : 4867
Authors : Ford KA, Gulevich AG, Swenson TL, Casida JE.
Abstract : Neonicotinoids not only control insect pests but also sometimes independently alter plant growth and response to stress. We find that imidacloprid, thiacloprid, acetamiprid, thiamethoxam, and clothianidin but not nitenpyram and dinotefuran induce foliar lesions and peroxidative damage in soybean ( Glycine max ) seedlings assayed with the 3,3'-diaminobenzidine stain. The chloropyridinyl-carboxylic acid (COOH) but not the -carboxaldehyde (CHO) metabolites induce peroxidative damage but in a different pattern. Surprisingly, the chlorothiazolyl -CHO and -COOH metabolites induce chlorosis but no clear superimposable peroxidative damage or cell death. Four metallo-oxidases known to modulate reactive oxygen species were not sensitive in vitro to the parent neonicotinoid itself but were to several CHO and COOH metabolites and related compounds, with a sensitivity order of CHO > COOH and tyrosinase > xanthine oxidase and aldehyde oxidase > catalase. Although metallo-oxidase inhibition does not correlate overall with lesion formation, it may play an as yet unknown role in plant response to neonicotinoids.
Phytotoxicity against Zea mays (maize) seedlings assessed as lesions at 50 to 100 ppm after 9 days
|
Zea mays
|
None
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: oxidative stress in planta and metallo-oxidase inhibition.
Year : 2011
Volume : 59
Issue : 9
First Page : 4860
Last Page : 4867
Authors : Ford KA, Gulevich AG, Swenson TL, Casida JE.
Abstract : Neonicotinoids not only control insect pests but also sometimes independently alter plant growth and response to stress. We find that imidacloprid, thiacloprid, acetamiprid, thiamethoxam, and clothianidin but not nitenpyram and dinotefuran induce foliar lesions and peroxidative damage in soybean ( Glycine max ) seedlings assayed with the 3,3'-diaminobenzidine stain. The chloropyridinyl-carboxylic acid (COOH) but not the -carboxaldehyde (CHO) metabolites induce peroxidative damage but in a different pattern. Surprisingly, the chlorothiazolyl -CHO and -COOH metabolites induce chlorosis but no clear superimposable peroxidative damage or cell death. Four metallo-oxidases known to modulate reactive oxygen species were not sensitive in vitro to the parent neonicotinoid itself but were to several CHO and COOH metabolites and related compounds, with a sensitivity order of CHO > COOH and tyrosinase > xanthine oxidase and aldehyde oxidase > catalase. Although metallo-oxidase inhibition does not correlate overall with lesion formation, it may play an as yet unknown role in plant response to neonicotinoids.
Phytotoxicity against Gossypium hirsutum (cotton) seedlings assessed as lesions at 50 to 100 ppm after 9 days
|
Gossypium hirsutum
|
None
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: oxidative stress in planta and metallo-oxidase inhibition.
Year : 2011
Volume : 59
Issue : 9
First Page : 4860
Last Page : 4867
Authors : Ford KA, Gulevich AG, Swenson TL, Casida JE.
Abstract : Neonicotinoids not only control insect pests but also sometimes independently alter plant growth and response to stress. We find that imidacloprid, thiacloprid, acetamiprid, thiamethoxam, and clothianidin but not nitenpyram and dinotefuran induce foliar lesions and peroxidative damage in soybean ( Glycine max ) seedlings assayed with the 3,3'-diaminobenzidine stain. The chloropyridinyl-carboxylic acid (COOH) but not the -carboxaldehyde (CHO) metabolites induce peroxidative damage but in a different pattern. Surprisingly, the chlorothiazolyl -CHO and -COOH metabolites induce chlorosis but no clear superimposable peroxidative damage or cell death. Four metallo-oxidases known to modulate reactive oxygen species were not sensitive in vitro to the parent neonicotinoid itself but were to several CHO and COOH metabolites and related compounds, with a sensitivity order of CHO > COOH and tyrosinase > xanthine oxidase and aldehyde oxidase > catalase. Although metallo-oxidase inhibition does not correlate overall with lesion formation, it may play an as yet unknown role in plant response to neonicotinoids.
Phytotoxicity against Glycine max (soybean) seedlings assessed as lesions in unfoliolate leaves at 100 ppm after 9 days
|
Glycine max
|
None
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: oxidative stress in planta and metallo-oxidase inhibition.
Year : 2011
Volume : 59
Issue : 9
First Page : 4860
Last Page : 4867
Authors : Ford KA, Gulevich AG, Swenson TL, Casida JE.
Abstract : Neonicotinoids not only control insect pests but also sometimes independently alter plant growth and response to stress. We find that imidacloprid, thiacloprid, acetamiprid, thiamethoxam, and clothianidin but not nitenpyram and dinotefuran induce foliar lesions and peroxidative damage in soybean ( Glycine max ) seedlings assayed with the 3,3'-diaminobenzidine stain. The chloropyridinyl-carboxylic acid (COOH) but not the -carboxaldehyde (CHO) metabolites induce peroxidative damage but in a different pattern. Surprisingly, the chlorothiazolyl -CHO and -COOH metabolites induce chlorosis but no clear superimposable peroxidative damage or cell death. Four metallo-oxidases known to modulate reactive oxygen species were not sensitive in vitro to the parent neonicotinoid itself but were to several CHO and COOH metabolites and related compounds, with a sensitivity order of CHO > COOH and tyrosinase > xanthine oxidase and aldehyde oxidase > catalase. Although metallo-oxidase inhibition does not correlate overall with lesion formation, it may play an as yet unknown role in plant response to neonicotinoids.
Displacement of fluorescent probe 1-NPN from Acyrthosiphon pisum (pea aphid) recombinant OBP3 by competitive binding assay
|
Acyrthosiphon pisum
|
None
|
|
Journal : J Agric Food Chem
Year : 2011
Volume : 59
Issue : 6
First Page : 2456
Last Page : 2461
Risk quotient, recommended field rate (g/ha) to LC50 for Trichogramma nubilale (mg/L)
|
Trichogramma nubilale
|
1.78
|
|
Journal : Crop Protection
Title : Susceptibility of adult Trichogramma nubilale (Hymenoptera: Trichogrammatidae) to selected insecticides with different modes of action
Year : 2012
Volume : 34
First Page : 76
Last Page : 72
Authors : Wang Y, Yu R, Zhao X, Chen L, Wu C, Cang T, Wang Q.
Abstract : The parasitic wasp Trichogramma nubilale (Hymenoptera: Trichogrammatidae) is one of the most suitable parasitoids for controlling Asian corn borer, Ostrinia furnacalis (Lepidoptera: Crambidae). Although extensive toxicological tests have been carried out to elucidate the toxicities of insecticides to trichogrammatids, the acute toxicity risks of commonly used insecticides to T. nubilale are not well known. Among the 7 classes of tested chemicals, organophosphates and carbamates had the highest intrinsic toxicity to the parasitoid with LC50 values ranging from 0.081 (0.062–0.12) to 2.10 (1.23–3.47) and from 0.12 (0.11–0.14) to 0.95 (0.87–1.05) mg a.i. per liter, respectively. The phenylpyrazoles (with the exception of butene-fipronil), avermectins, neonicotinoids and pyrethroids induced intermediate toxicity responses with LC50 values ranging from 0.29 to 4.67, 2.36 to 11.27, 1.86 to 311.9, and 10.98–150.3 mg a.i. per liter, respectively. In contrast, insect growth regulators (IGRs) exhibited the least toxicity to the parasitoid with LC50 values ranging from 3452 (3114–3877) to 10,168 (8848–12,027) mg a.i. per liter. A risk quotient analysis indicated that neonicotinoids, avermectins, pyrethroids, IGRs and phenylpyrazoles (with the exception of butene-fipronil) were safe, but organophosphates and carbamates were slightly to moderately toxic or highly toxic to T. nubilale. This study provided informative data for implementing both biological and chemical control strategies in integrated pest management (IPM) of corn lepidopterans.
Contact toxicity against Trichogramma nubilale assessed as mortality after 24 hr by modified slight dry film method
|
Trichogramma nubilale
|
461.2
mgAi/L
|
|
Contact toxicity against Trichogramma nubilale assessed as mortality after 24 hr by modified slight dry film method
|
Trichogramma nubilale
|
56.73
mgAi/L
|
|
Journal : Crop Protection
Title : Susceptibility of adult Trichogramma nubilale (Hymenoptera: Trichogrammatidae) to selected insecticides with different modes of action
Year : 2012
Volume : 34
First Page : 76
Last Page : 72
Authors : Wang Y, Yu R, Zhao X, Chen L, Wu C, Cang T, Wang Q.
Abstract : The parasitic wasp Trichogramma nubilale (Hymenoptera: Trichogrammatidae) is one of the most suitable parasitoids for controlling Asian corn borer, Ostrinia furnacalis (Lepidoptera: Crambidae). Although extensive toxicological tests have been carried out to elucidate the toxicities of insecticides to trichogrammatids, the acute toxicity risks of commonly used insecticides to T. nubilale are not well known. Among the 7 classes of tested chemicals, organophosphates and carbamates had the highest intrinsic toxicity to the parasitoid with LC50 values ranging from 0.081 (0.062–0.12) to 2.10 (1.23–3.47) and from 0.12 (0.11–0.14) to 0.95 (0.87–1.05) mg a.i. per liter, respectively. The phenylpyrazoles (with the exception of butene-fipronil), avermectins, neonicotinoids and pyrethroids induced intermediate toxicity responses with LC50 values ranging from 0.29 to 4.67, 2.36 to 11.27, 1.86 to 311.9, and 10.98–150.3 mg a.i. per liter, respectively. In contrast, insect growth regulators (IGRs) exhibited the least toxicity to the parasitoid with LC50 values ranging from 3452 (3114–3877) to 10,168 (8848–12,027) mg a.i. per liter. A risk quotient analysis indicated that neonicotinoids, avermectins, pyrethroids, IGRs and phenylpyrazoles (with the exception of butene-fipronil) were safe, but organophosphates and carbamates were slightly to moderately toxic or highly toxic to T. nubilale. This study provided informative data for implementing both biological and chemical control strategies in integrated pest management (IPM) of corn lepidopterans.
Binding affinity to freshwater snail Lymnaea stagnalis AChBP assessed as [3H]EPI binding by radioligand binding assay
|
Lymnaea stagnalis
|
220.0
nM
|
|
Journal : J Agric Food Chem
Title : Unique neonicotinoid binding conformations conferring selective receptor interactions.
Year : 2011
Volume : 59
Issue : 7
First Page : 2825
Last Page : 2828
Authors : Tomizawa M, Casida JE.
Abstract : Neonicotinoid agonists selectively act on the insect nicotinic acetylcholine receptor (nAChR). The molecular basis for this specificity is deciphered by comparisons of two acetylcholine binding proteins (AChBPs) with distinct pharmacological profiles that serve as structural homologues for the nAChR subtypes. Aplysia AChBP has high neonicotinoid sensitivity, whereas Lymnaea AChBP has low neonicotinoid sensitivity, pharmacologies reminiscent of insect and vertebrate nAChR subtypes, respectively. The ligand-receptor interactions for these AChBPs were established by chemical and structural neurobiology approaches. Neonicotinoids and nicotinoids bind in a single conformation with Aplysia AChBP, wherein the electronegative nitro or cyano pharmacophore of the neonicotinoid faces in a reversed orientation relative to the cationic nicotinoid functionality. For Lymnaea AChBP, the neonicotinoids have two binding conformations in this vertebrate receptor model, which are completely inverted relative to each other, whereas nicotinoids are nestled in only one conserved conformation. Therefore, the unique binding conformations of nicotinic agonists determine the selective receptor interactions.
Binding affinity to salt water mollusc Aplysia californica AChBP Y55W mutant assessed as [3H]acetamiprid binding by radioligand binding assay
|
Aplysia californica
|
3.9
nM
|
|
Journal : J Agric Food Chem
Title : Unique neonicotinoid binding conformations conferring selective receptor interactions.
Year : 2011
Volume : 59
Issue : 7
First Page : 2825
Last Page : 2828
Authors : Tomizawa M, Casida JE.
Abstract : Neonicotinoid agonists selectively act on the insect nicotinic acetylcholine receptor (nAChR). The molecular basis for this specificity is deciphered by comparisons of two acetylcholine binding proteins (AChBPs) with distinct pharmacological profiles that serve as structural homologues for the nAChR subtypes. Aplysia AChBP has high neonicotinoid sensitivity, whereas Lymnaea AChBP has low neonicotinoid sensitivity, pharmacologies reminiscent of insect and vertebrate nAChR subtypes, respectively. The ligand-receptor interactions for these AChBPs were established by chemical and structural neurobiology approaches. Neonicotinoids and nicotinoids bind in a single conformation with Aplysia AChBP, wherein the electronegative nitro or cyano pharmacophore of the neonicotinoid faces in a reversed orientation relative to the cationic nicotinoid functionality. For Lymnaea AChBP, the neonicotinoids have two binding conformations in this vertebrate receptor model, which are completely inverted relative to each other, whereas nicotinoids are nestled in only one conserved conformation. Therefore, the unique binding conformations of nicotinic agonists determine the selective receptor interactions.
Binding affinity to recombinant Gallus gallus (chicken) alpha4beta2 nicotinic acetylcholine receptor assessed as [3H]NIC binding by radioligand binding assay
|
Gallus gallus
|
240.0
nM
|
|
Journal : J Agric Food Chem
Title : Unique neonicotinoid binding conformations conferring selective receptor interactions.
Year : 2011
Volume : 59
Issue : 7
First Page : 2825
Last Page : 2828
Authors : Tomizawa M, Casida JE.
Abstract : Neonicotinoid agonists selectively act on the insect nicotinic acetylcholine receptor (nAChR). The molecular basis for this specificity is deciphered by comparisons of two acetylcholine binding proteins (AChBPs) with distinct pharmacological profiles that serve as structural homologues for the nAChR subtypes. Aplysia AChBP has high neonicotinoid sensitivity, whereas Lymnaea AChBP has low neonicotinoid sensitivity, pharmacologies reminiscent of insect and vertebrate nAChR subtypes, respectively. The ligand-receptor interactions for these AChBPs were established by chemical and structural neurobiology approaches. Neonicotinoids and nicotinoids bind in a single conformation with Aplysia AChBP, wherein the electronegative nitro or cyano pharmacophore of the neonicotinoid faces in a reversed orientation relative to the cationic nicotinoid functionality. For Lymnaea AChBP, the neonicotinoids have two binding conformations in this vertebrate receptor model, which are completely inverted relative to each other, whereas nicotinoids are nestled in only one conserved conformation. Therefore, the unique binding conformations of nicotinic agonists determine the selective receptor interactions.
Binding affinity to Drosophila brain nicotinic acetylcholine receptor assessed as [3H]IMI binding by radioligand binding assay
|
Drosophila
|
1.2
nM
|
|
Journal : J Agric Food Chem
Title : Unique neonicotinoid binding conformations conferring selective receptor interactions.
Year : 2011
Volume : 59
Issue : 7
First Page : 2825
Last Page : 2828
Authors : Tomizawa M, Casida JE.
Abstract : Neonicotinoid agonists selectively act on the insect nicotinic acetylcholine receptor (nAChR). The molecular basis for this specificity is deciphered by comparisons of two acetylcholine binding proteins (AChBPs) with distinct pharmacological profiles that serve as structural homologues for the nAChR subtypes. Aplysia AChBP has high neonicotinoid sensitivity, whereas Lymnaea AChBP has low neonicotinoid sensitivity, pharmacologies reminiscent of insect and vertebrate nAChR subtypes, respectively. The ligand-receptor interactions for these AChBPs were established by chemical and structural neurobiology approaches. Neonicotinoids and nicotinoids bind in a single conformation with Aplysia AChBP, wherein the electronegative nitro or cyano pharmacophore of the neonicotinoid faces in a reversed orientation relative to the cationic nicotinoid functionality. For Lymnaea AChBP, the neonicotinoids have two binding conformations in this vertebrate receptor model, which are completely inverted relative to each other, whereas nicotinoids are nestled in only one conserved conformation. Therefore, the unique binding conformations of nicotinic agonists determine the selective receptor interactions.
Retention time under basic conditions using 20 mM Na2HPO4 (pH9.9)/MeOH (1:1) mobile phase by HPLC method
|
None
|
6.05
min
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors.
Year : 2000
Volume : 48
Issue : 12
First Page : 6016
Last Page : 6024
Authors : Tomizawa M, Lee DL, Casida JE.
Abstract : The favorable selective toxicity of neonicotinoid insecticides (represented here by imidacloprid, thiacloprid, and a nitromethylene analogue) for insects versus mammals is not shared by three of their N-unsubstituted imine derivatives or by nicotine or epibatidine. The same selectivity pattern is evident at the receptor level, i.e., the insect nicotinic acetylcholine receptor (nAChR) versus mammalian nAChR subtypes (alpha1, alpha3, alpha4, and alpha7) assayed independently. The insect-selective compounds are not protonated with a nitroimine, cyanoimine, or nitromethylene group and the mammalian-selective compounds are ionized at physiological pH. We propose that the negatively charged tip of the nitro or cyano group (not a partial positive charge at imidazolidine N-1 as suggested earlier) interacts with a putative cationic subsite of the insect nAChR. This contrasts with the mammalian nAChRs where the iminium cation (+C-NH2 <--> C =+NH2) of the neonicotinoid imine derivatives or ammonium nitrogen of nicotine or epibatidine interacts with the anionic subsite.
Retention time under acidic conditions using H20/MeOH mobile phase containing 0.1% TFA (1:1) by HPLC method
|
None
|
6.07
min
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors.
Year : 2000
Volume : 48
Issue : 12
First Page : 6016
Last Page : 6024
Authors : Tomizawa M, Lee DL, Casida JE.
Abstract : The favorable selective toxicity of neonicotinoid insecticides (represented here by imidacloprid, thiacloprid, and a nitromethylene analogue) for insects versus mammals is not shared by three of their N-unsubstituted imine derivatives or by nicotine or epibatidine. The same selectivity pattern is evident at the receptor level, i.e., the insect nicotinic acetylcholine receptor (nAChR) versus mammalian nAChR subtypes (alpha1, alpha3, alpha4, and alpha7) assayed independently. The insect-selective compounds are not protonated with a nitroimine, cyanoimine, or nitromethylene group and the mammalian-selective compounds are ionized at physiological pH. We propose that the negatively charged tip of the nitro or cyano group (not a partial positive charge at imidazolidine N-1 as suggested earlier) interacts with a putative cationic subsite of the insect nAChR. This contrasts with the mammalian nAChRs where the iminium cation (+C-NH2 <--> C =+NH2) of the neonicotinoid imine derivatives or ammonium nitrogen of nicotine or epibatidine interacts with the anionic subsite.
Retention time under neutral conditions using H20/MeOH (1:1) mobile phase by HPLC method
|
None
|
6.06
min
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors.
Year : 2000
Volume : 48
Issue : 12
First Page : 6016
Last Page : 6024
Authors : Tomizawa M, Lee DL, Casida JE.
Abstract : The favorable selective toxicity of neonicotinoid insecticides (represented here by imidacloprid, thiacloprid, and a nitromethylene analogue) for insects versus mammals is not shared by three of their N-unsubstituted imine derivatives or by nicotine or epibatidine. The same selectivity pattern is evident at the receptor level, i.e., the insect nicotinic acetylcholine receptor (nAChR) versus mammalian nAChR subtypes (alpha1, alpha3, alpha4, and alpha7) assayed independently. The insect-selective compounds are not protonated with a nitroimine, cyanoimine, or nitromethylene group and the mammalian-selective compounds are ionized at physiological pH. We propose that the negatively charged tip of the nitro or cyano group (not a partial positive charge at imidazolidine N-1 as suggested earlier) interacts with a putative cationic subsite of the insect nAChR. This contrasts with the mammalian nAChRs where the iminium cation (+C-NH2 <--> C =+NH2) of the neonicotinoid imine derivatives or ammonium nitrogen of nicotine or epibatidine interacts with the anionic subsite.
Inhibition of [3H]nicotine binding to alpha4 nicotinic acetylcholine receptor in Mus musculus (mouse) M10 cells co-expressing beta2 nicotinic acetylcholine receptor subunits
|
Mus musculus
|
860.0
nM
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors.
Year : 2000
Volume : 48
Issue : 12
First Page : 6016
Last Page : 6024
Authors : Tomizawa M, Lee DL, Casida JE.
Abstract : The favorable selective toxicity of neonicotinoid insecticides (represented here by imidacloprid, thiacloprid, and a nitromethylene analogue) for insects versus mammals is not shared by three of their N-unsubstituted imine derivatives or by nicotine or epibatidine. The same selectivity pattern is evident at the receptor level, i.e., the insect nicotinic acetylcholine receptor (nAChR) versus mammalian nAChR subtypes (alpha1, alpha3, alpha4, and alpha7) assayed independently. The insect-selective compounds are not protonated with a nitroimine, cyanoimine, or nitromethylene group and the mammalian-selective compounds are ionized at physiological pH. We propose that the negatively charged tip of the nitro or cyano group (not a partial positive charge at imidazolidine N-1 as suggested earlier) interacts with a putative cationic subsite of the insect nAChR. This contrasts with the mammalian nAChRs where the iminium cation (+C-NH2 <--> C =+NH2) of the neonicotinoid imine derivatives or ammonium nitrogen of nicotine or epibatidine interacts with the anionic subsite.
Inhibition of [3H]nicotine binding to alpha3 nicotinic acetylcholine receptor in Homo sapiens (human) SH-SY5Y cells co-expressing beta2beta4alpha5 Nicotinic acetylcholine receptor subunits
|
Homo sapiens
|
None
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors.
Year : 2000
Volume : 48
Issue : 12
First Page : 6016
Last Page : 6024
Authors : Tomizawa M, Lee DL, Casida JE.
Abstract : The favorable selective toxicity of neonicotinoid insecticides (represented here by imidacloprid, thiacloprid, and a nitromethylene analogue) for insects versus mammals is not shared by three of their N-unsubstituted imine derivatives or by nicotine or epibatidine. The same selectivity pattern is evident at the receptor level, i.e., the insect nicotinic acetylcholine receptor (nAChR) versus mammalian nAChR subtypes (alpha1, alpha3, alpha4, and alpha7) assayed independently. The insect-selective compounds are not protonated with a nitroimine, cyanoimine, or nitromethylene group and the mammalian-selective compounds are ionized at physiological pH. We propose that the negatively charged tip of the nitro or cyano group (not a partial positive charge at imidazolidine N-1 as suggested earlier) interacts with a putative cationic subsite of the insect nAChR. This contrasts with the mammalian nAChRs where the iminium cation (+C-NH2 <--> C =+NH2) of the neonicotinoid imine derivatives or ammonium nitrogen of nicotine or epibatidine interacts with the anionic subsite.
Inhibition of [3H]alpha-BGT binding to alpha7 nicotinic acetylcholine receptor in Homo sapiens (human) SH-SY5Y cells
|
Homo sapiens
|
100000.0
nM
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors.
Year : 2000
Volume : 48
Issue : 12
First Page : 6016
Last Page : 6024
Authors : Tomizawa M, Lee DL, Casida JE.
Abstract : The favorable selective toxicity of neonicotinoid insecticides (represented here by imidacloprid, thiacloprid, and a nitromethylene analogue) for insects versus mammals is not shared by three of their N-unsubstituted imine derivatives or by nicotine or epibatidine. The same selectivity pattern is evident at the receptor level, i.e., the insect nicotinic acetylcholine receptor (nAChR) versus mammalian nAChR subtypes (alpha1, alpha3, alpha4, and alpha7) assayed independently. The insect-selective compounds are not protonated with a nitroimine, cyanoimine, or nitromethylene group and the mammalian-selective compounds are ionized at physiological pH. We propose that the negatively charged tip of the nitro or cyano group (not a partial positive charge at imidazolidine N-1 as suggested earlier) interacts with a putative cationic subsite of the insect nAChR. This contrasts with the mammalian nAChRs where the iminium cation (+C-NH2 <--> C =+NH2) of the neonicotinoid imine derivatives or ammonium nitrogen of nicotine or epibatidine interacts with the anionic subsite.
Inhibition of [3H]alpha-BGT binding to alpha1 nicotinic acetylcholine receptor in Homo sapiens (human) TE671 cells co-expressing gammaalpha1deltabeta1 nicotinic acetylcholine receptor subunits
|
Homo sapiens
|
120000.0
nM
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors.
Year : 2000
Volume : 48
Issue : 12
First Page : 6016
Last Page : 6024
Authors : Tomizawa M, Lee DL, Casida JE.
Abstract : The favorable selective toxicity of neonicotinoid insecticides (represented here by imidacloprid, thiacloprid, and a nitromethylene analogue) for insects versus mammals is not shared by three of their N-unsubstituted imine derivatives or by nicotine or epibatidine. The same selectivity pattern is evident at the receptor level, i.e., the insect nicotinic acetylcholine receptor (nAChR) versus mammalian nAChR subtypes (alpha1, alpha3, alpha4, and alpha7) assayed independently. The insect-selective compounds are not protonated with a nitroimine, cyanoimine, or nitromethylene group and the mammalian-selective compounds are ionized at physiological pH. We propose that the negatively charged tip of the nitro or cyano group (not a partial positive charge at imidazolidine N-1 as suggested earlier) interacts with a putative cationic subsite of the insect nAChR. This contrasts with the mammalian nAChRs where the iminium cation (+C-NH2 <--> C =+NH2) of the neonicotinoid imine derivatives or ammonium nitrogen of nicotine or epibatidine interacts with the anionic subsite.
Toxicity against Musca domestica (house fly) dosed with compound through intra-thoracic injection pre-treated with 100 ug/g metabolic detoxification inhibitor O-propyl O-(2-propynyl)phenylphosphonate
|
Musca domestica
|
0.03
mg.kg-1
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors.
Year : 2000
Volume : 48
Issue : 12
First Page : 6016
Last Page : 6024
Authors : Tomizawa M, Lee DL, Casida JE.
Abstract : The favorable selective toxicity of neonicotinoid insecticides (represented here by imidacloprid, thiacloprid, and a nitromethylene analogue) for insects versus mammals is not shared by three of their N-unsubstituted imine derivatives or by nicotine or epibatidine. The same selectivity pattern is evident at the receptor level, i.e., the insect nicotinic acetylcholine receptor (nAChR) versus mammalian nAChR subtypes (alpha1, alpha3, alpha4, and alpha7) assayed independently. The insect-selective compounds are not protonated with a nitroimine, cyanoimine, or nitromethylene group and the mammalian-selective compounds are ionized at physiological pH. We propose that the negatively charged tip of the nitro or cyano group (not a partial positive charge at imidazolidine N-1 as suggested earlier) interacts with a putative cationic subsite of the insect nAChR. This contrasts with the mammalian nAChRs where the iminium cation (+C-NH2 <--> C =+NH2) of the neonicotinoid imine derivatives or ammonium nitrogen of nicotine or epibatidine interacts with the anionic subsite.
Toxicity in ip dosed Mus musculus (mouse)
|
Mus musculus
|
25.0
mg.kg-1
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors.
Year : 2000
Volume : 48
Issue : 12
First Page : 6016
Last Page : 6024
Authors : Tomizawa M, Lee DL, Casida JE.
Abstract : The favorable selective toxicity of neonicotinoid insecticides (represented here by imidacloprid, thiacloprid, and a nitromethylene analogue) for insects versus mammals is not shared by three of their N-unsubstituted imine derivatives or by nicotine or epibatidine. The same selectivity pattern is evident at the receptor level, i.e., the insect nicotinic acetylcholine receptor (nAChR) versus mammalian nAChR subtypes (alpha1, alpha3, alpha4, and alpha7) assayed independently. The insect-selective compounds are not protonated with a nitroimine, cyanoimine, or nitromethylene group and the mammalian-selective compounds are ionized at physiological pH. We propose that the negatively charged tip of the nitro or cyano group (not a partial positive charge at imidazolidine N-1 as suggested earlier) interacts with a putative cationic subsite of the insect nAChR. This contrasts with the mammalian nAChRs where the iminium cation (+C-NH2 <--> C =+NH2) of the neonicotinoid imine derivatives or ammonium nitrogen of nicotine or epibatidine interacts with the anionic subsite.
Inhibition of [3H]IMI binding to Drosophila melanogaster neuronal acetylcholine receptor
|
Drosophila melanogaster
|
2.7
nM
|
|
Journal : J Agric Food Chem
Title : Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors.
Year : 2000
Volume : 48
Issue : 12
First Page : 6016
Last Page : 6024
Authors : Tomizawa M, Lee DL, Casida JE.
Abstract : The favorable selective toxicity of neonicotinoid insecticides (represented here by imidacloprid, thiacloprid, and a nitromethylene analogue) for insects versus mammals is not shared by three of their N-unsubstituted imine derivatives or by nicotine or epibatidine. The same selectivity pattern is evident at the receptor level, i.e., the insect nicotinic acetylcholine receptor (nAChR) versus mammalian nAChR subtypes (alpha1, alpha3, alpha4, and alpha7) assayed independently. The insect-selective compounds are not protonated with a nitroimine, cyanoimine, or nitromethylene group and the mammalian-selective compounds are ionized at physiological pH. We propose that the negatively charged tip of the nitro or cyano group (not a partial positive charge at imidazolidine N-1 as suggested earlier) interacts with a putative cationic subsite of the insect nAChR. This contrasts with the mammalian nAChRs where the iminium cation (+C-NH2 <--> C =+NH2) of the neonicotinoid imine derivatives or ammonium nitrogen of nicotine or epibatidine interacts with the anionic subsite.
Displacement of [3H]IMI from nicotinic acetylcholine receptor in Drosophila melanogaster head membrane after 90 min by filter binding assay
|
Drosophila melanogaster
|
7.5
nM
|
|
Journal : J. Neurochem.
Year : 2000
Volume : 75
Issue : 3
First Page : 1294
Last Page : 1303
Displacement of [3H]IMI from nicotinic acetylcholine receptor in Myzus persicae (green peach aphid) whole body membrane after 90 min by filter binding assay
|
Myzus persicae
|
3.4
nM
|
|
Journal : J. Neurochem.
Year : 2000
Volume : 75
Issue : 3
First Page : 1294
Last Page : 1303
Ratio of EC50 for Daphnia magna to EC50 for first instar larvae of Cheumatopsyche brevilineata
|
None
|
3.63
|
|
Journal : J Pesticide Sci
Title : A useful new insecticide bioassay using first-instar larvae of a net-spinning caddisfly, Cheumatopsyche brevilineata (Trichoptera: Hydropsychidae)
Year : 2009
Volume : 34
Issue : 1
First Page : 13
Last Page : 20
Authors : Yokoyama A, Ohtsu K, Iwafune T, Nagai T, Ishihara S, Kobara Y, Horio T, Endo S
Insecticidal activity against first-instar larvae of Cheumatopsyche brevilineata after 48 hr
|
Cheumatopsyche
|
0.00527
ug.mL-1
|
|
Journal : J Pesticide Sci
Title : A useful new insecticide bioassay using first-instar larvae of a net-spinning caddisfly, Cheumatopsyche brevilineata (Trichoptera: Hydropsychidae)
Year : 2009
Volume : 34
Issue : 1
First Page : 13
Last Page : 20
Authors : Yokoyama A, Ohtsu K, Iwafune T, Nagai T, Ishihara S, Kobara Y, Horio T, Endo S
Octanol-water partition coefficient, log KOW of the compound
|
None
|
1.26
|
|
Journal : J Pesticide Sci
Title : A useful new insecticide bioassay using first-instar larvae of a net-spinning caddisfly, Cheumatopsyche brevilineata (Trichoptera: Hydropsychidae)
Year : 2009
Volume : 34
Issue : 1
First Page : 13
Last Page : 20
Authors : Yokoyama A, Ohtsu K, Iwafune T, Nagai T, Ishihara S, Kobara Y, Horio T, Endo S
Insecticidal activity against Daphnia magna after 48 hr
|
Daphnia magna
|
22.52
ug.mL-1
|
|
Journal : J Pesticide Sci
Title : A useful new insecticide bioassay using first-instar larvae of a net-spinning caddisfly, Cheumatopsyche brevilineata (Trichoptera: Hydropsychidae)
Year : 2009
Volume : 34
Issue : 1
First Page : 13
Last Page : 20
Authors : Yokoyama A, Ohtsu K, Iwafune T, Nagai T, Ishihara S, Kobara Y, Horio T, Endo S
Resistance factor, ratio of LC50 for adult female Bemisia tabaci B-biotype NJ-Imi (sweet potato whitefly) (G30) to LC50 for adult female B-type Bemisia tabaci NJ
|
Bemisia tabaci
|
37.0
|
|
Journal : Pest Manag Sci
Title : Cross-resistance, inheritance and biochemical mechanisms of imidacloprid resistance in B-biotype Bemisia tabaci.
Year : 2009
Volume : 65
Issue : 11
First Page : 1189
Last Page : 1194
Authors : Wang Z, Yao M, Wu Y.
Abstract : BACKGROUND: The B-type Bemisia tabaci (Gennadius) has become established in many regions in China, and neonicotinoids are extensively used to control this pest. Imidacloprid resistance in a laboratory-selected strain of B-type B. tabaci was characterised in order to provide the basis for recommending resistance management tactics. RESULTS: The NJ-Imi strain of B-type B. tabaci was selected from the NJ strain with imidacloprid for 30 generations. The NJ-Imi strain exhibited 490-fold resistance to imidacloprid, high levels of cross-resistance to three other neonicotinoids, low levels of cross-resistance to monosultap, cartap and spinosad, but no cross-resistance to abamectin and cypermethrin. Imidacloprid resistance in the NJ-Imi strain was autosomal and semi-dominant. It is shown that enhanced detoxification mediated by cytochrome-P450-dependent monooxygenases contributes to imidacloprid resistance to some extent in the NJ-Imi strain. Results from synergist bioassays and cross-resistance patterns indicated that target-site insensitivity may be involved in imidacloprid resistance in the NJ-Imi strain of B. tabaci. CONCLUSION: Although oxidative detoxification mediated by P450 monooxygenases is involved in imidacloprid resistance in the NJ-Imi strain of B-type B. tabaci, target-site modification as an additional resistance mechanism cannot be ruled out. Considering the high risk of cross-resistance, neonicotinoids should be regarded as a single group when implementing an insecticide rotation scheme in B. tabaci control.
Insecticidal activity against adult female imidacloprid-resistant Bemisia tabaci B-biotype NJ-Imi (sweet potato whitefly) (G30) in cotton leaf discs assessed as mortality treated for 10 secs prior to adult infestation measured after 72 hr by leaf-dip bioassay
|
Bemisia tabaci
|
37.3
ug.mL-1
|
|
Journal : Pest Manag Sci
Title : Cross-resistance, inheritance and biochemical mechanisms of imidacloprid resistance in B-biotype Bemisia tabaci.
Year : 2009
Volume : 65
Issue : 11
First Page : 1189
Last Page : 1194
Authors : Wang Z, Yao M, Wu Y.
Abstract : BACKGROUND: The B-type Bemisia tabaci (Gennadius) has become established in many regions in China, and neonicotinoids are extensively used to control this pest. Imidacloprid resistance in a laboratory-selected strain of B-type B. tabaci was characterised in order to provide the basis for recommending resistance management tactics. RESULTS: The NJ-Imi strain of B-type B. tabaci was selected from the NJ strain with imidacloprid for 30 generations. The NJ-Imi strain exhibited 490-fold resistance to imidacloprid, high levels of cross-resistance to three other neonicotinoids, low levels of cross-resistance to monosultap, cartap and spinosad, but no cross-resistance to abamectin and cypermethrin. Imidacloprid resistance in the NJ-Imi strain was autosomal and semi-dominant. It is shown that enhanced detoxification mediated by cytochrome-P450-dependent monooxygenases contributes to imidacloprid resistance to some extent in the NJ-Imi strain. Results from synergist bioassays and cross-resistance patterns indicated that target-site insensitivity may be involved in imidacloprid resistance in the NJ-Imi strain of B. tabaci. CONCLUSION: Although oxidative detoxification mediated by P450 monooxygenases is involved in imidacloprid resistance in the NJ-Imi strain of B-type B. tabaci, target-site modification as an additional resistance mechanism cannot be ruled out. Considering the high risk of cross-resistance, neonicotinoids should be regarded as a single group when implementing an insecticide rotation scheme in B. tabaci control.
Insecticidal activity against adult female imidacloprid-susceptible Bemisia tabaci B-biotype NJ (sweet potato whitefly) in cotton leaf discs assessed as mortality treated for 10 secs prior to adult infestation measured after 72 hr by leaf-dip bioassay
|
Bemisia tabaci
|
1.02
ug.mL-1
|
|
Journal : Pest Manag Sci
Title : Cross-resistance, inheritance and biochemical mechanisms of imidacloprid resistance in B-biotype Bemisia tabaci.
Year : 2009
Volume : 65
Issue : 11
First Page : 1189
Last Page : 1194
Authors : Wang Z, Yao M, Wu Y.
Abstract : BACKGROUND: The B-type Bemisia tabaci (Gennadius) has become established in many regions in China, and neonicotinoids are extensively used to control this pest. Imidacloprid resistance in a laboratory-selected strain of B-type B. tabaci was characterised in order to provide the basis for recommending resistance management tactics. RESULTS: The NJ-Imi strain of B-type B. tabaci was selected from the NJ strain with imidacloprid for 30 generations. The NJ-Imi strain exhibited 490-fold resistance to imidacloprid, high levels of cross-resistance to three other neonicotinoids, low levels of cross-resistance to monosultap, cartap and spinosad, but no cross-resistance to abamectin and cypermethrin. Imidacloprid resistance in the NJ-Imi strain was autosomal and semi-dominant. It is shown that enhanced detoxification mediated by cytochrome-P450-dependent monooxygenases contributes to imidacloprid resistance to some extent in the NJ-Imi strain. Results from synergist bioassays and cross-resistance patterns indicated that target-site insensitivity may be involved in imidacloprid resistance in the NJ-Imi strain of B. tabaci. CONCLUSION: Although oxidative detoxification mediated by P450 monooxygenases is involved in imidacloprid resistance in the NJ-Imi strain of B-type B. tabaci, target-site modification as an additional resistance mechanism cannot be ruled out. Considering the high risk of cross-resistance, neonicotinoids should be regarded as a single group when implementing an insecticide rotation scheme in B. tabaci control.
Toxicity against Metaseiulus occidentalis adults in bean leaf disk infested with two-spotted spider mites assessed as repellency at 0.1333 g AI/L treated using worst-case laboratory exposure procedure measured after 72 hr (Rvb = 16.1%)
|
Metaseiulus occidentalis
|
49.4
%
|
|
Journal : Pest Manag Sci
Year : 2009
Volume : 65
Issue : 6
First Page : 635
Last Page : 639
Toxicity against Metaseiulus occidentalis adults in bean leaf disk infested with two-spotted spider mites assessed as repellency at 0.1333 g AI/L treated using worst-case laboratory exposure procedure measured after 48 hr (Rvb = 13.6%)
|
Metaseiulus occidentalis
|
44.9
%
|
|
Journal : Pest Manag Sci
Year : 2009
Volume : 65
Issue : 6
First Page : 635
Last Page : 639
Toxicity against Metaseiulus occidentalis adults in bean leaf disk infested with two-spotted spider mites assessed as repellency at 0.1333 g AI/L treated using worst-case laboratory exposure procedure measured after 24 hr (Rvb = 3.6%)
|
Metaseiulus occidentalis
|
12.2
%
|
|
Journal : Pest Manag Sci
Year : 2009
Volume : 65
Issue : 6
First Page : 635
Last Page : 639
Toxicity against Metaseiulus occidentalis adults in bean leaf disk infested with two-spotted spider mites assessed as average number of eggs laid (fecundity) at 0.1333 g AI/L treated using worst-case laboratory exposure procedure measured after 72 hr (Rvb = 2.23/day)
|
Metaseiulus occidentalis
|
1.58
/day
|
|
Journal : Pest Manag Sci
Year : 2009
Volume : 65
Issue : 6
First Page : 635
Last Page : 639
Toxicity against Metaseiulus occidentalis adults in bean leaf disk infested with two-spotted spider mites assessed as average number of eggs laid (fecundity) at 0.1333 g AI/L treated using worst-case laboratory exposure procedure measured after 48 hr (Rvb = 2.30/day)
|
Metaseiulus occidentalis
|
1.26
/day
|
|
Journal : Pest Manag Sci
Year : 2009
Volume : 65
Issue : 6
First Page : 635
Last Page : 639
Toxicity against Metaseiulus occidentalis adults in bean leaf disk infested with two-spotted spider mites assessed as average number of eggs laid (fecundity) at 0.1333 g AI/L treated using worst-case laboratory exposure procedure measured after 24 hr (Rvb = 2.11/day)
|
Metaseiulus occidentalis
|
1.64
/day
|
|
Journal : Pest Manag Sci
Year : 2009
Volume : 65
Issue : 6
First Page : 635
Last Page : 639
Toxicity against Metaseiulus occidentalis adults in bean leaf disk infested with two-spotted spider mites assessed as corrected mortality at 0.1600 g AI/L treated using worst-case laboratory exposure procedure measured after 72 hr
|
Metaseiulus occidentalis
|
2.8
%
|
|
Journal : Pest Manag Sci
Year : 2009
Volume : 65
Issue : 6
First Page : 635
Last Page : 639
Toxicity against Metaseiulus occidentalis adults in bean leaf disk infested with two-spotted spider mites assessed as corrected mortality at 2x0.1600 g AI/L treated using worst-case laboratory exposure procedure measured after 72 hr
|
Metaseiulus occidentalis
|
2.3
%
|
|
Journal : Pest Manag Sci
Year : 2009
Volume : 65
Issue : 6
First Page : 635
Last Page : 639
Toxicity against Metaseiulus occidentalis adults in bean leaf disk infested with two-spotted spider mites assessed as corrected mortality at 4x0.1600 g AI/L treated using worst-case laboratory exposure procedure measured after 72 hr
|
Metaseiulus occidentalis
|
5.8
%
|
|
Journal : Pest Manag Sci
Year : 2009
Volume : 65
Issue : 6
First Page : 635
Last Page : 639
Ovicidal activity against Metaseiulus occidentalis eggs in bean leaf disk infested with two-spotted spider mites assessed as corrected cumulative mortality at 480 g/L SC formulation treated using worst-case laboratory exposure procedure measured after 144 hr (Rvb = 0.7%)
|
Metaseiulus occidentalis
|
1.9
%
|
|
Journal : Pest Manag Sci
Year : 2009
Volume : 65
Issue : 6
First Page : 635
Last Page : 639
Resistance index, ratio of LC50 for neonicotinoid-resistant Myzus persicae FRC-P (green peach aphid) to LC50 for Myzus persicae 4106A
|
Myzus persicae
|
2500.0
|
|
Journal : Pest Manag Sci
Title : Investigating the mode of action of sulfoxaflor: a fourth-generation neonicotinoid.
Year : 2013
Volume : 69
Issue : 5
First Page : 607
Last Page : 619
Authors : Cutler P, Slater R, Edmunds AJ, Maienfisch P, Hall RG, Earley FG, Pitterna T, Pal S, Paul VL, Goodchild J, Blacker M, Hagmann L, Crossthwaite AJ.
Abstract : The precise mode of action of sulfoxaflor, a new nicotinic acetylcholine receptor-modulating insecticide, is unclear. A detailed understanding of the mode of action, especially in relation to the neonicotinoids, is essential for recommending effective pest management practices.Radiolabel binding experiments using a tritiated analogue of sulfoxaflor ([(3) H]-methyl-SFX) performed on membranes from Myzus persicae demonstrate that sulfoxaflor interacts specifically with the high-affinity imidacloprid binding site present in a subpopulation of the total nAChR pool. In competition studies, imidacloprid-like neonicotinoids displace [(3) H]-methyl-SFX at pM concentrations. The effects of sulfoxaflor on the exposed aphid nervous system in situ are analogous to those of imidacloprid and nitenpyram, and finally the high-affinity sulfoxaflor binding site is absent in a Myzus persicae strain (clone FRC) possessing a single amino acid point mutation (R81T) in the β-nAChR, a region critical for neonicotinoid interaction.The nicotinic acetylcholine receptor pharmacological profile of sulfoxaflor in aphids is consistent with that of imidacloprid. Additionally, the insecticidal activity of sulfoxaflor and the current commercialised neonicotinoids is affected by the point mutation in FRC Myzus persicae. Therefore, it is suggested that sulfoxalfor be considered a neonicotinoid, and that this be taken into account when recommending insecticide rotation partnering for effective resistance management programmes.
Insecticidal activity against Myzus persicae 4106A (green peach aphid) fed on compound treated chinese cabbage discs after 72 hr
|
Myzus persicae
|
0.4
ppm
|
|
Journal : Pest Manag Sci
Title : Investigating the mode of action of sulfoxaflor: a fourth-generation neonicotinoid.
Year : 2013
Volume : 69
Issue : 5
First Page : 607
Last Page : 619
Authors : Cutler P, Slater R, Edmunds AJ, Maienfisch P, Hall RG, Earley FG, Pitterna T, Pal S, Paul VL, Goodchild J, Blacker M, Hagmann L, Crossthwaite AJ.
Abstract : The precise mode of action of sulfoxaflor, a new nicotinic acetylcholine receptor-modulating insecticide, is unclear. A detailed understanding of the mode of action, especially in relation to the neonicotinoids, is essential for recommending effective pest management practices.Radiolabel binding experiments using a tritiated analogue of sulfoxaflor ([(3) H]-methyl-SFX) performed on membranes from Myzus persicae demonstrate that sulfoxaflor interacts specifically with the high-affinity imidacloprid binding site present in a subpopulation of the total nAChR pool. In competition studies, imidacloprid-like neonicotinoids displace [(3) H]-methyl-SFX at pM concentrations. The effects of sulfoxaflor on the exposed aphid nervous system in situ are analogous to those of imidacloprid and nitenpyram, and finally the high-affinity sulfoxaflor binding site is absent in a Myzus persicae strain (clone FRC) possessing a single amino acid point mutation (R81T) in the β-nAChR, a region critical for neonicotinoid interaction.The nicotinic acetylcholine receptor pharmacological profile of sulfoxaflor in aphids is consistent with that of imidacloprid. Additionally, the insecticidal activity of sulfoxaflor and the current commercialised neonicotinoids is affected by the point mutation in FRC Myzus persicae. Therefore, it is suggested that sulfoxalfor be considered a neonicotinoid, and that this be taken into account when recommending insecticide rotation partnering for effective resistance management programmes.
Insecticidal activity against neonicotinoid-resistant Myzus persicae FRC-P (green peach aphid) fed on compound treated chinese cabbage discs after 72 hr
|
Myzus persicae
|
1000.0
ppm
|
|
Journal : Pest Manag Sci
Title : Investigating the mode of action of sulfoxaflor: a fourth-generation neonicotinoid.
Year : 2013
Volume : 69
Issue : 5
First Page : 607
Last Page : 619
Authors : Cutler P, Slater R, Edmunds AJ, Maienfisch P, Hall RG, Earley FG, Pitterna T, Pal S, Paul VL, Goodchild J, Blacker M, Hagmann L, Crossthwaite AJ.
Abstract : The precise mode of action of sulfoxaflor, a new nicotinic acetylcholine receptor-modulating insecticide, is unclear. A detailed understanding of the mode of action, especially in relation to the neonicotinoids, is essential for recommending effective pest management practices.Radiolabel binding experiments using a tritiated analogue of sulfoxaflor ([(3) H]-methyl-SFX) performed on membranes from Myzus persicae demonstrate that sulfoxaflor interacts specifically with the high-affinity imidacloprid binding site present in a subpopulation of the total nAChR pool. In competition studies, imidacloprid-like neonicotinoids displace [(3) H]-methyl-SFX at pM concentrations. The effects of sulfoxaflor on the exposed aphid nervous system in situ are analogous to those of imidacloprid and nitenpyram, and finally the high-affinity sulfoxaflor binding site is absent in a Myzus persicae strain (clone FRC) possessing a single amino acid point mutation (R81T) in the β-nAChR, a region critical for neonicotinoid interaction.The nicotinic acetylcholine receptor pharmacological profile of sulfoxaflor in aphids is consistent with that of imidacloprid. Additionally, the insecticidal activity of sulfoxaflor and the current commercialised neonicotinoids is affected by the point mutation in FRC Myzus persicae. Therefore, it is suggested that sulfoxalfor be considered a neonicotinoid, and that this be taken into account when recommending insecticide rotation partnering for effective resistance management programmes.
Displacement of [3H]IMD from nAChR in Myzus persicae 4106A (green peach aphid) membrane after 70 min
|
Myzus persicae
|
0.17
nM
|
|
Journal : Pest Manag Sci
Title : Investigating the mode of action of sulfoxaflor: a fourth-generation neonicotinoid.
Year : 2013
Volume : 69
Issue : 5
First Page : 607
Last Page : 619
Authors : Cutler P, Slater R, Edmunds AJ, Maienfisch P, Hall RG, Earley FG, Pitterna T, Pal S, Paul VL, Goodchild J, Blacker M, Hagmann L, Crossthwaite AJ.
Abstract : The precise mode of action of sulfoxaflor, a new nicotinic acetylcholine receptor-modulating insecticide, is unclear. A detailed understanding of the mode of action, especially in relation to the neonicotinoids, is essential for recommending effective pest management practices.Radiolabel binding experiments using a tritiated analogue of sulfoxaflor ([(3) H]-methyl-SFX) performed on membranes from Myzus persicae demonstrate that sulfoxaflor interacts specifically with the high-affinity imidacloprid binding site present in a subpopulation of the total nAChR pool. In competition studies, imidacloprid-like neonicotinoids displace [(3) H]-methyl-SFX at pM concentrations. The effects of sulfoxaflor on the exposed aphid nervous system in situ are analogous to those of imidacloprid and nitenpyram, and finally the high-affinity sulfoxaflor binding site is absent in a Myzus persicae strain (clone FRC) possessing a single amino acid point mutation (R81T) in the β-nAChR, a region critical for neonicotinoid interaction.The nicotinic acetylcholine receptor pharmacological profile of sulfoxaflor in aphids is consistent with that of imidacloprid. Additionally, the insecticidal activity of sulfoxaflor and the current commercialised neonicotinoids is affected by the point mutation in FRC Myzus persicae. Therefore, it is suggested that sulfoxalfor be considered a neonicotinoid, and that this be taken into account when recommending insecticide rotation partnering for effective resistance management programmes.
Displacement of [3H]-methyl-SFX from nAChR in Myzus persicae 4106A (green peach aphid) membrane after 70 min
|
Myzus persicae
|
0.041
nM
|
|
Journal : Pest Manag Sci
Title : Investigating the mode of action of sulfoxaflor: a fourth-generation neonicotinoid.
Year : 2013
Volume : 69
Issue : 5
First Page : 607
Last Page : 619
Authors : Cutler P, Slater R, Edmunds AJ, Maienfisch P, Hall RG, Earley FG, Pitterna T, Pal S, Paul VL, Goodchild J, Blacker M, Hagmann L, Crossthwaite AJ.
Abstract : The precise mode of action of sulfoxaflor, a new nicotinic acetylcholine receptor-modulating insecticide, is unclear. A detailed understanding of the mode of action, especially in relation to the neonicotinoids, is essential for recommending effective pest management practices.Radiolabel binding experiments using a tritiated analogue of sulfoxaflor ([(3) H]-methyl-SFX) performed on membranes from Myzus persicae demonstrate that sulfoxaflor interacts specifically with the high-affinity imidacloprid binding site present in a subpopulation of the total nAChR pool. In competition studies, imidacloprid-like neonicotinoids displace [(3) H]-methyl-SFX at pM concentrations. The effects of sulfoxaflor on the exposed aphid nervous system in situ are analogous to those of imidacloprid and nitenpyram, and finally the high-affinity sulfoxaflor binding site is absent in a Myzus persicae strain (clone FRC) possessing a single amino acid point mutation (R81T) in the β-nAChR, a region critical for neonicotinoid interaction.The nicotinic acetylcholine receptor pharmacological profile of sulfoxaflor in aphids is consistent with that of imidacloprid. Additionally, the insecticidal activity of sulfoxaflor and the current commercialised neonicotinoids is affected by the point mutation in FRC Myzus persicae. Therefore, it is suggested that sulfoxalfor be considered a neonicotinoid, and that this be taken into account when recommending insecticide rotation partnering for effective resistance management programmes.
Octanol-water partition coefficient, log P of the compound at 23 degC by shake flask method
|
None
|
1.2
|
|
Journal : J Pesticide Sci
Year : 2002
Volume : 27
Issue : 3
First Page : 267
Last Page : 271
Insecticidal activity against Periplaneta americana (American cockroach) assessed as killing compound injected into abdomen of cockroach after 24 hr in presence of 50 ug piperonyl butoxide oxidative metabolism inhibitor and 50 ug propargyl propyl benzenephosphonate inhibitor of hydrolytic
|
Periplaneta americana
|
0.21
nmol
|
|
Journal : J Pesticide Sci
Year : 2002
Volume : 27
Issue : 3
First Page : 267
Last Page : 271
Insecticidal activity against Periplaneta americana (American cockroach) assessed as neuroblocking concentration
|
Periplaneta americana
|
2.6
uM
|
|
Journal : J Pesticide Sci
Year : 2002
Volume : 27
Issue : 3
First Page : 267
Last Page : 271
Insecticidal activity against Periplaneta americana (American cockroach) assessed as killing compound injected into abdomen of cockroach after 24 hr in presence of 50 ug propargyl propyl benzenephosphonate inhibitor of hydrolytic metabolism of tetramethrin pyrethroid
|
Periplaneta americana
|
0.46
nmol
|
|
Journal : J Pesticide Sci
Year : 2002
Volume : 27
Issue : 3
First Page : 267
Last Page : 271
Insecticidal activity against Periplaneta americana (American cockroach) assessed as killing compound injected into abdomen of cockroach after 24 hr in presence of 50 ug piperonyl butoxide oxidative metabolism inhibitor
|
Periplaneta americana
|
5.9
nmol
|
|
Journal : J Pesticide Sci
Year : 2002
Volume : 27
Issue : 3
First Page : 267
Last Page : 271
Insecticidal activity against Periplaneta americana (American cockroach) assessed as killing compound injected into abdomen of cockroach after 24 hr
|
Periplaneta americana
|
21.0
nmol
|
|
Journal : J Pesticide Sci
Year : 2002
Volume : 27
Issue : 3
First Page : 267
Last Page : 271
Insecticidal activity against imidacloprid-resistant Aphis gossypii (cotton aphid) in cotton leaves assessed as fecundity at LC20 concentration
|
Aphis gossypii
|
None
|
|
Journal : Pest Manag Sci
Year : 2011
Volume : 67
Issue : 12
First Page : 1528
Last Page : 1533
Insecticidal activity against imidacloprid-resistant Aphis gossypii (cotton aphid) in cotton leaves assessed as longevity at LC20 concentration
|
Aphis gossypii
|
10.6
day
|
|
Journal : Pest Manag Sci
Year : 2011
Volume : 67
Issue : 12
First Page : 1528
Last Page : 1533
Insecticidal activity against imidacloprid-resistant Aphis gossypii (cotton aphid) in cotton leaves assessed as inhibition of honeydew excretion at LC20 concentration measured after 72 hr by dipping method
|
Aphis gossypii
|
36.9
%
|
|
Journal : Pest Manag Sci
Year : 2011
Volume : 67
Issue : 12
First Page : 1528
Last Page : 1533
Insecticidal activity against imidacloprid-resistant Aphis gossypii (cotton aphid) in cotton leaves assessed as reduction in body weight at LC20 concentration measured after 72 hr by dipping method (Rvb = 0.40 +/- 0.0002 mg/aphid)
|
Aphis gossypii
|
0.16
mg
|
|
Journal : Pest Manag Sci
Year : 2011
Volume : 67
Issue : 12
First Page : 1528
Last Page : 1533
Insecticidal activity against imidacloprid-resistant Aphis gossypii (cotton aphid) in cotton leaves assessed as reduction in body weight at LC20 concentration measured after 48 hr by dipping method (Rvb = 0.36 +/- 0.0006 mg/aphid)
|
Aphis gossypii
|
0.18
mg
|
|
Journal : Pest Manag Sci
Year : 2011
Volume : 67
Issue : 12
First Page : 1528
Last Page : 1533
Insecticidal activity against imidacloprid-resistant Aphis gossypii (cotton aphid) in cotton leaves assessed as mortality measured after 72 hr by dipping method
|
Aphis gossypii
|
5.45
ug ml-1
|
|
Journal : Pest Manag Sci
Year : 2011
Volume : 67
Issue : 12
First Page : 1528
Last Page : 1533
Insecticidal activity against imidacloprid-resistant Aphis gossypii (cotton aphid) in cotton leaves assessed as reduction in body weight at LC20 concentration measured after 24 hr by dipping method (Rvb = 0.33 +/- 0.0004 mg/aphid)
|
Aphis gossypii
|
0.19
mg
|
|
Journal : Pest Manag Sci
Year : 2011
Volume : 67
Issue : 12
First Page : 1528
Last Page : 1533
Resistance ratio, LC50 for Aphis gossypii RF45 (cotton aphid) to LC50 for Aphis gossypii SS
|
Aphis gossypii
|
3.68
|
|
Journal : Pest Manag Sci
Year : 2011
Volume : 67
Issue : 12
First Page : 1528
Last Page : 1533
Insecticidal activity against imidacloprid-resistant Aphis gossypii RF45 (cotton aphid) in cotton leaves assessed as mortality measured after 48 hr by dipping method
|
Aphis gossypii
|
8.69
microg/mL2
|
|
Journal : Pest Manag Sci
Year : 2011
Volume : 67
Issue : 12
First Page : 1528
Last Page : 1533
Insecticidal activity against Aphis gossypii SS (cotton aphid) in cotton leaves assessed as mortality measured after 48 hr by dipping method
|
Aphis gossypii
|
2.36
microg/mL2
|
|
Journal : Pest Manag Sci
Year : 2011
Volume : 67
Issue : 12
First Page : 1528
Last Page : 1533
Insecticidal activity against Frankliniella occidentalis SPI5 (western flower thrips) in compound treated sweet pepper leaf assessed as mortality at 216 mg/l at 25 +/- 2 degC by leaf dip method
|
Frankliniella occidentalis
|
3.3
%
|
|
Journal : Pest Manag Sci
Title : Thiamethoxam acts as a target-site synergist of spinosad in resistant strains of Frankliniella occidentalis.
Year : 2013
Volume : 69
Issue : 2
First Page : 188
Last Page : 194
Authors : Guillén J, Bielza P.
Abstract : Previous studies have suggested that the resistance mechanism towards spinosad in Frankliniella occidentalis (Pergande) is an altered target site. Like the neonicotinoids, the spinosyns act on nicotinic acetylcholine receptors (nAChRs) in insects, but at a distinct site. The changes in nAChRs related to spinosad resistance in thrips might involve interaction with neonicotinoids. In this study, the efficacy of spinosad and neonicotinoids, alone and in combination, was evaluated in susceptible and spinosad-resistant thrips strains.The neonicotinoids tested were imidacloprid, thiacloprid, acetamiprid, thiamethoxam and clothianidin. No cross-resistance was shown between spinosad and any of the neonicotinoids. However, an increased toxicity was observed when a mixture of spinosad with thiamethoxam or clothianidin was tested. No synergism was found in the susceptible strains. The more spinosad-resistant the thrips strain, the stronger was the synergism.Data suggest that spinosad and thiamethoxam may interact at the nAChRs in spinosad-resistant thrips, facilitating enhanced insecticidal action.
Insecticidal activity against Frankliniella occidentalis TFA (western flower thrips) in compound treated sweet pepper leaf assessed as mortality at 216 mg/l at 25 +/- 2 degC by leaf dip method
|
Frankliniella occidentalis
|
3.3
%
|
|
Journal : Pest Manag Sci
Title : Thiamethoxam acts as a target-site synergist of spinosad in resistant strains of Frankliniella occidentalis.
Year : 2013
Volume : 69
Issue : 2
First Page : 188
Last Page : 194
Authors : Guillén J, Bielza P.
Abstract : Previous studies have suggested that the resistance mechanism towards spinosad in Frankliniella occidentalis (Pergande) is an altered target site. Like the neonicotinoids, the spinosyns act on nicotinic acetylcholine receptors (nAChRs) in insects, but at a distinct site. The changes in nAChRs related to spinosad resistance in thrips might involve interaction with neonicotinoids. In this study, the efficacy of spinosad and neonicotinoids, alone and in combination, was evaluated in susceptible and spinosad-resistant thrips strains.The neonicotinoids tested were imidacloprid, thiacloprid, acetamiprid, thiamethoxam and clothianidin. No cross-resistance was shown between spinosad and any of the neonicotinoids. However, an increased toxicity was observed when a mixture of spinosad with thiamethoxam or clothianidin was tested. No synergism was found in the susceptible strains. The more spinosad-resistant the thrips strain, the stronger was the synergism.Data suggest that spinosad and thiamethoxam may interact at the nAChRs in spinosad-resistant thrips, facilitating enhanced insecticidal action.
Insecticidal activity against Frankliniella occidentalis R1 (western flower thrips) in compound treated sweet pepper leaf assessed as mortality at 216 mg/l at 25 +/- 2 degC by leaf dip method
|
Frankliniella occidentalis
|
0.0
%
|
|
Journal : Pest Manag Sci
Title : Thiamethoxam acts as a target-site synergist of spinosad in resistant strains of Frankliniella occidentalis.
Year : 2013
Volume : 69
Issue : 2
First Page : 188
Last Page : 194
Authors : Guillén J, Bielza P.
Abstract : Previous studies have suggested that the resistance mechanism towards spinosad in Frankliniella occidentalis (Pergande) is an altered target site. Like the neonicotinoids, the spinosyns act on nicotinic acetylcholine receptors (nAChRs) in insects, but at a distinct site. The changes in nAChRs related to spinosad resistance in thrips might involve interaction with neonicotinoids. In this study, the efficacy of spinosad and neonicotinoids, alone and in combination, was evaluated in susceptible and spinosad-resistant thrips strains.The neonicotinoids tested were imidacloprid, thiacloprid, acetamiprid, thiamethoxam and clothianidin. No cross-resistance was shown between spinosad and any of the neonicotinoids. However, an increased toxicity was observed when a mixture of spinosad with thiamethoxam or clothianidin was tested. No synergism was found in the susceptible strains. The more spinosad-resistant the thrips strain, the stronger was the synergism.Data suggest that spinosad and thiamethoxam may interact at the nAChRs in spinosad-resistant thrips, facilitating enhanced insecticidal action.
Insecticidal activity against Frankliniella occidentalis TFB (western flower thrips) in compound treated sweet pepper leaf assessed as mortality at 216 mg/l at 25 +/- 2 degC by leaf dip method
|
Frankliniella occidentalis
|
10.0
%
|
|
Journal : Pest Manag Sci
Title : Thiamethoxam acts as a target-site synergist of spinosad in resistant strains of Frankliniella occidentalis.
Year : 2013
Volume : 69
Issue : 2
First Page : 188
Last Page : 194
Authors : Guillén J, Bielza P.
Abstract : Previous studies have suggested that the resistance mechanism towards spinosad in Frankliniella occidentalis (Pergande) is an altered target site. Like the neonicotinoids, the spinosyns act on nicotinic acetylcholine receptors (nAChRs) in insects, but at a distinct site. The changes in nAChRs related to spinosad resistance in thrips might involve interaction with neonicotinoids. In this study, the efficacy of spinosad and neonicotinoids, alone and in combination, was evaluated in susceptible and spinosad-resistant thrips strains.The neonicotinoids tested were imidacloprid, thiacloprid, acetamiprid, thiamethoxam and clothianidin. No cross-resistance was shown between spinosad and any of the neonicotinoids. However, an increased toxicity was observed when a mixture of spinosad with thiamethoxam or clothianidin was tested. No synergism was found in the susceptible strains. The more spinosad-resistant the thrips strain, the stronger was the synergism.Data suggest that spinosad and thiamethoxam may interact at the nAChRs in spinosad-resistant thrips, facilitating enhanced insecticidal action.