Matsumura F, Ghiasuddin S M
J Environ Sci Health B. 1983;18(1):1-14. doi: 10.1080/03601238309372355.
Evidence has been obtained to indicate that cyclodiene-type insecticides, e.g., heptachlor epoxide and gamma-BHC, mimic the action of picrotoxinin. These insecticides inhibit the GABA (gamma-aminobutyric acid)-stimulated chloride uptake in the coxal muscle of the American cockroach, and directly compete against [3H]a-dihydropicrotoxinin for binding in the rat brain synaptosomes. Moreover, several cyclodiene-resistant insect strains are also resistant to picrotoxinin. This cross-resistance is specific to picrotoxinin and does not extend to other neuroexcitants. These insecticides, like picrotoxinin, cause central nerve excitation by stimulating transmitter release. Similarity in molecular structures also has been pointed out. These results indicate that some of the nerve excitation symptoms that insecticides cause are likely due to their interaction with picrotoxinin receptor.
已有证据表明，环二烯类杀虫剂，如环氧七氯和γ-六氯环己烷，可模拟印防己毒素的作用。这些杀虫剂抑制美国蟑螂髋部肌肉中γ-氨基丁酸（GABA）刺激的氯离子摄取，并在大鼠脑突触体中与[3H]α-二氢印防己毒素直接竞争结合位点。此外，几种对环二烯类杀虫剂有抗性的昆虫品系对印防己毒素也有抗性。这种交叉抗性对印防己毒素具有特异性，并不扩展到其他神经兴奋剂。这些杀虫剂与印防己毒素一样，通过刺激递质释放引起中枢神经兴奋。分子结构上的相似性也已被指出。这些结果表明，杀虫剂引起的一些神经兴奋症状可能是由于它们与印防己毒素受体的相互作用所致。
