By U. Eder, H. C. von Keyserlingk (auth.), Dr. Harald C. von Keyserlingk, Dr. Albert Jäger, Dr. Christoph von Szczepanski (eds.)
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Extra resources for Approaches to New Leads for Insecticides
1978). Both sulfoxides and sulfones may readily carbamoylate endogenous sulfhydryl groups such as those present in glutathione and CoASR. Similarly, a sulfhydryl-containing enzyme in the JR biosynthetic pathway could be inhibited, resulting in AJR manifestations (Kramer et al. 1982). Experiments in which the bisthiolcarbamate at 10- 4 M was incubated with cultured corpora allata from M. sexta together with [14C]-methionine showed 100% inhibition of JR biosynthesis (Kramer et al. 1982 and 1983).
For an inseeticide like earbofuran the peak eoneentration that a toxic dose of earbofuran reaehes is somewhere in the region of 10- 5 M (Collins et al. 1983). Now for earbofuran to be toxic, it ean be present at slighdy less than that, but really we are dealing with the mieromolar range or above in a praetieal sense. It is not neeessary for a eompound to be aetive in the nanomolar range to be inseeticidal. So, when designing eompounds or looking for aetivity, the mieromolar range is a reasonable figure to eonsider.
The same thing was true of tetrodotoxin; an ED so of 89 vs. A. Miller Table 3. Bioassay of sodium channel drugs on third instar larvae, Musca domestica by the thermal stimulus-response method. 0· • Dose giving 50% paralysis 10min after treatment b Tetrodotoxin values for ED so are in pg • Significant differences between strains fected by procaine or tetrodotoxin is not altered in this kdr strain. 6 ~g versus far greater than 10). Components of scorpion venom that are suspected to act on certain parts of the sodium channel show a similar bioassay response, so what the kdr gene has done to the sodium channel alters responses to deltamethrin and aconitine but it does not affect responses to procaine, tetrodotoxin, and scorpion venom.