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Pyrethroids


A pyrethroid is an organic compound similar to the natural pyrethrins produced by the flowers of pyrethrums (Chrysanthemum cinerariaefolium and C. coccineum). Pyrethroids constitute the majority of commercial household insecticides. In the concentrations used in such products, they may also have insect repellent properties and are generally harmless to humans.

Pyrethroids are axonic excitoxins, the toxic effects of which are mediated through preventing the closure of the voltage-gated sodium channels in the axonal membranes. The sodium channel is a membrane protein with a hydrophilic interior. This interior is a tiny hole which is shaped precisely to strip away the partially charged water molecules from a sodium ion and create a favorable way for sodium ions to pass through the membrane, enter the axon, and propagate an action potential. When the toxin keeps the channels in their open state, the nerves cannot repolarize, leaving the axonal membrane permanently depolarized, thereby paralyzing the organism.

Pyrethroids can be combined with the synergist piperonyl butoxide, a known inhibitor of key microsomal enzymes from metabolizing the pyrethroid, which increases its efficacy (lethality).


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