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杀虫机制
MOA: GABA Antagonist Phenylpyrazole (fipronil), cyclodienes Antagonists of GABA activated chloride channels GABA Antagonists: chemicals that bind to but do not activate GAMMA-AMINOBUTYRIC ACID receptors, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID or GAMMA-AMINOBUTYRIC ACID agonists. GABA can’t bind to receptor Doesn’t activate channel (doesn’t open) Interferes with (prevents) the passage of chlorine ions through the channel. Concerns with cross resistance with other GABAergic insecticides * GABA GABA receptor GABA Receptor in Central Nervous System Phenylpyrazoles or Fiproles GABA-receptors GABA Chloride ions Fipronil * Phenyl pyrazoles Fipronil Chipco Choice -- mole crickets grubs Firestar, Ouver-N-Out, (Ceasefire)--fireants Termidor -- termites Regent -- corn Frontline -- flea tick MaxForce FC -- cockroaches and ants Most lipophilic insecticide ever discovered Persistent in soil Spread among social insects on bodies 4 months of residual on dogs (binds to oils in sebaceous glands) * MOA: GABA Agonist Avermectins Bind to GABA (Gamma-Amino-Butyric Acid gated chloride channel Opens channel Chloride influx Cannot reach threshold for action potential Causes membrane to hyperpolarize, making it less excitatory, decreasing nerve transmission Result: flaccid paralysis and death * Avermectins Abamectin Avert -- cockroaches Advance -- ants Produced from soil microbials. Stomach poison for ants and cockroaches slow acting low toxicity to mammals * Nervous System Why does this happen? Let’s look at a “normal” nerve impulse. * “Diagram of a neuron illustrating the subcellular locations of voltage-gated sodium channels.” #4. Myelinated #3. Unmyelinated #6. Apical dendrites #5. Presynaptic #7. Postsynaptic U of Colorado Health Science * Rensselar Polytechnic Institute Axon Membrane at Rest “Leaky membrane” K+: many leaky channels Na-: few leaky channels Outside: Na- Inside: K+ * Axon Membrane Rensselar Polytechnic Institute An
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