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Biochemical Sites of Insecticide Action and Resistance - Isaac Ishaaya

Biochemical Sites of Insecticide Action and Resistance

By: Isaac Ishaaya (Editor)

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  • Paperback View Product Published: 19th September 2011
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The authors of this book report up-to-date methodologies relating to isolation, identification and use of various enzymes and receptor systems that serve as targets for insecticide action or as sites for resistance development. Thus, this book serves as an indispensable tool for scientists in academia and industry research, investigating or developing new insecticides with selective properties for the benefit of the environment. Possible countermeasures for resistance to novel insecticides are discussed.

Biochemical Processes Related to Insecticide Action: an Overview
Introductionp. 1
Chitin Synthesis Inhibitionp. 2
Ecdysone and Juvenile Hormone Receptorsp. 4
Acetylcholine Receptorsp. 5
GABA and Glutamate Receptors and Ion Channelsp. 6
Other Biochemical Sitesp. 8
Conclusionsp. 9
Referencesp. 10
GABA and Glutamate Receptors as Biochemical Sites for Insecticide Action
Introductionp. 17
GABA Receptors in Mammals and Insectsp. 18
Classification of GABA Receptorsp. 18
Structure and Physiological Role of Insect GABA Receptorsp. 18
Pharmacology of GABA Receptorsp. 19
Summary of Effects of Convulsants and Avermectins on the GABA Receptorp. 19
Polychlorocycloalkanes and Related Norbornanesp. 21
Picrodendrin and Silphinene Natural Productsp. 22
Fipronil and Fipronil Analogsp. 25
Trioxabicyclooctanes and Related Compoundsp. 27
New Avermectins and the Mammalian GABA Receptorp. 28
Altered GABA Receptors in Resistancep. 30
Resistance to New and Experimental Insecticidesp. 31
Glutamate-Gated Chloride Channelsp. 33
Physiology, Pharmacology, and Molecular Structurep. 33
Effects ofthe Avermectinsp. 34
New Avermectins and Their Usesp. 35
Target Site Resistance to the Avermectinsp. 36
Conclusionsp. 36
Referencesp. 37
Insecticides Affecting Voltage-Gated Ion Channels
Insecticides and Ion Channelsp. 43
Scope and Aimp. 43
Voltage-Gated Ion Channelsp. 44
Industrial Insecticides Targeting Ion Channelsp. 48
Insecticides of the Voltage-Gated Sodium Channelsp. 48
Insecticides of the Potassium and Calcium Channelsp. 52
The Functional Diversity of Insecticidesp. 54
Multiplicity of Effectsp. 54
Distinction Between Mammals and Insectsp. 56
Neurotoxic Polypeptidesp. 57
Animal Group Specificityp. 57
Insect-Selective Neurotoxins Affecting the Voltage-Gated Sodium Channelsp. 58
Scorpion Venom Toxinsp. 58
Spider Venom Toxinsp. 61
Insect-Selective Neurotoxins Affecting the Voltage-Gated Calcium Channelp. 61
Recombinant Baculovirus Bioinsecticidesp. 62
Allosteric Coupling and Allosteric Antagonismp. 64
Referencesp. 69
Acetylcholine Receptors as Sites for Developing Neonicotinoid Insecticides
Introductionp. 77
Insect Nicotinic Acetylcholine Receptorsp. 80
Structurep. 80
Diversityp. 80
Compounds Acting on the Nicotinic Acetylcholine Receptorp. 83
Radioligand Binding Studiesp. 83
Neonicotinoidsp. 86
Imidacloprid and Related Structuresp. 86
Mannich Adducts as Experimental Pro-Neonicotinoidsp. 91
Electrophysiological Considerationsp. 92
Whole Cell Voltage Clamp of Native Neuron Preparationsp. 94
Correlation Between Electrophysiology and Radioligand Binding Studiesp. 96
Agonists vs.Antagonistsp. 98
Receptor Subtypes in Locusta migratoriap. 99
Referencesp. 101
Ecdysteroid and Juvenile Hormone Receptors: Properties and Importance in Developing Novel Insecticides
Introductionp. 107
Ecdysteroidsp. 107
Biology, Endocrinology and Molecular Biologyp. 108
Receptors and Other Target Sitesp. 112
Non-Steroidal Ecdysone Analogs and Their Mode of Actionp. 115
Receptor-Based Screening Assaysp. 119
Future Directionsp. 120
Juvenile Hormonep. 121
Biology, Endocrinology and Molecular Biologyp. 121
Receptors and Other Target Sitesp. 122
JH Analogs and Their Modes of Actionp. 125
Receptor-Based Screening Assaysp. 126
Future Directionsp. 126
Referencesp. 127
Imaginal Discs and Tissue Cultures as Targets for Insecticide Action
Introductionp. 133
Imaginal Discs as Targets of Insect Hormones in Vivo and in Vitrop. 133
Insecticide Action in Vitro: Juvenile Hormone Mimicsp. 136
Insecticide Action in Vitro: Chitin Synthesis Inhibitorsp. 137
Organ Culturesp. 137
Cell Linesp. 139
Insecticide Action in Vitro: Ecdysteroid Agonistsp. 139
Organ Culturesp. 139
Cell Linesp. 140
Referencesp. 145
Insect Neuropeptide Antagonists: a Novel Approach for Insect Control
Introductionp. 151
Backbone Cyclic Neuropeptide-Based Antagonist (BBC-NBA) Approachp. 153
Determination of the Active Sequence in the Neuropeptidep. 153
Development of a Competitive Lead Antagonistp. 154
Improvement of the Antagonistic Activity by Conformational Constraintp. 155
Backbone Cyclization: a Tool for Imposing Conformational Constraint on Peptidesp. 156
Cycloscan: Conformationally Constrained BBC Peptide Librariesp. 156
Pheromone Biosynthesis Activating Neuropeptidep. 158
Implementation of the BBC-NBA Strategy to the Pyrokinin/PBAN Familyp. 159
Conversion of Neuropeptide Antagonists into Insecticide Prototypesp. 160
Concluding Remarksp. 161
Referencesp. 163
Ion Balance in the Lepidopteran Midgut and Insecticidal Action of Bacillus thuringiensis
Introductionp. 167
Pathogenesisp. 168
Dependence of Host and Pathogen on Midgut pHp. 169
Midgut K+ and H+ Regulationp. 170
The K+ Pumpp. 170
The 2K+/1ATP Model for Midgut Alkalizationp. 171
The 1K+/1ATP Model for Midgut Alkalizationp. 173
Transmembrane and Transepithelial Ion Gradientsp. 175
Disruption of Midgut Ion Homeostasis by Bacillus thuringiensisp. 176
In Vivo Changesp. 176
In Vitro Changesp. 179
What is the Source of the Elevated Hemolymph K+?p. 181
Larval Paralysis and Mortality Factorsp. 182
-Endotoxin Effects on K+-Dependent Uptake of Amino Acidsp. 182
Correlating -Endotoxin Effects on the Isolated Midgut with Insecticidal Activityp. 185
Receptor Binding and Ion-Channel Formationp. 186
Receptor Bindingp. 186
Ion-Channel Formation in Artificial Membranes and BBMVsp. 188
Insect Cell Lines as Proxies for Midgut Cells In Vivop. 190
Membrane Insertion and Pore Formationp. 192
Conclusions and Thoughtsp. 196
Referencesp. 197
Evolution of Amplified Esterase Genes as a Mode of Insecticide Resistance In Aphids
Introductionp. 209
Biochemistry of Esterase-Based Resistance in M.persicaep. 210
Molecular Genetics of Esterase Overproductionp. 210
Esterase Genes in Susceptible Aphidsp. 211
Organization of Amplified Esterase Genesp. 212
Cytogenetic Studies of Amplified Esterasesp. 213
Expression of Esterase Genesp. 215
Wider Implicationsp. 216
Referencesp. 217
Insensitive Acetylcholinesterase as Sites for Resistance to Organophosphates and Carbamates in Insects: Insensitive Acetylcholinesterase Confers Resistance in Lepidoptera
Introductionp. 221
Acetylcholinesterase as a Resistance Mechanismp. 222
Insensitive AChE in Lepidopteran Speciesp. 224
Insensitive AChE in H. punctigerap. 225
Forms of AChE in Lepidopterap. 226
Effects of Altered AChE on Acetylcholine Hydrolysisp. 229
Inhibition Ratios and Toxicity in Lepidopterap. 230
Cross Resistance Between Organophosphates and Carbamates in Lepidopterap. 231
Genetics of Resistance in Lepidopterap. 231
Fitness of Resistance in Lepidopterap. 232
Evolutionp. 233
Control of Altered AChE in Lepidopterap. 233
Population Genetics and Monitoringp. 234
Conclusionsp. 235
Referencesp. 236
Glutathione S-Transferases and Insect Resistance to Insecticides
Introductionp. 239
General Features of Glutathione S-Transferases (GSTs)p. 239
Rolesp. 239
Biochemical and Physiological Characteristicsp. 240
Structure, Regulation, and Evolution of GST Genesp. 241
Insect GSTsp. 242
Rolesp. 242
Biochemical and Physiological Characteristicsp. 243
GSTs and Insecticide Resistancep. 244
Molecular Biology Studiesp. 245
GST Studies of Several Insectsp. 246
Drosophila melanogasterp. 246
Musca domesticap. 246
Anopheles gambiaep. 247
Plutella xylostellap. 248
Concluding Remarksp. 251
Referencesp. 252
Cytochrome P450 Monooxygenases and Insecticide Resistance: Lessons from CYP6D1
Cytochrome P450 Monooxygenasesp. 255
Insecticide Resistancep. 256
Monooxygenase-Mediated Insecticide Resistancep. 256
CYP6D1 and Insecticide Resistancep. 257
Summary of the Lessons Learned from CYP6D1p. 261
Referencesp. 263
Mechanisms of Organophosphate Resistance in Insects
Introductionp. 269
Physiological Mechanisms of Resistancep. 270
Resistance Mechanisms Involving Enhanced Biotransformationp. 272
Cytochrome-P450-Dependent Monooxygenasesp. 272
Glutathione S-Transferasesp. 274
Hydrolytic Enzymesp. 276
Quantitative Changes (Gene Amplification)p. 277
Qualitative Changesp. 281
Target Site Insensitivityp. 283
Interactions Between Resistance Mechanismsp. 284
Summaryp. 286
Referencesp. 287
Insect Midgut as a Site for Insecticide Detoxification and Resistance
Introductionp. 293
The Insect Gut: a Natural Digestive-Absorption Architecturep. 294
Enzymatic Metabolism of Pesticide Involved in Resistancep. 298
Impact of Ingestion, and Penetration and Disposition in the Insect Body on Resistance to Pesticidesp. 304
Attempts for Chemical Modeling of Digestion and Absorption in Insect Midgutp. 310
In Vitro Gut Cultures for Insecticidal Activity Studiesp. 314
Referencesp. 316
Impact of Insecticide Resistance Mechanisms on Management Strategies
Introductionp. 323
Overview of Resistance Mechanismsp. 324
Overview of Resistance Management Tacticsp. 325
Diagnosing Resistancep. 327
In Vitro Assays for Diagnosing Resistancep. 328
Overpowering Resistance Mechanismsp. 331
Resolving and Exploiting Cross-Resistancep. 332
Conclusionsp. 334
Referencesp. 335
Subject Indexp. 339
Table of Contents provided by Publisher. All Rights Reserved.

ISBN: 9783540676256
ISBN-10: 3540676252
Audience: Professional
Format: Hardcover
Language: English
Number Of Pages: 343
Publisher: Springer-Verlag Berlin and Heidelberg Gmbh & Co. Kg
Country of Publication: DE
Dimensions (cm): 23.5 x 16.51  x 1.91
Weight (kg): 0.64