Evidence for similarities between cyclodiene type insecticides and picrotoxinin in their action mechanisms.
Evidence for similarities between cyclodiene type insecticides and picrotoxinin in their action mechanisms.
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DOI：
10.1080/03601238309372355
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发表时间：
1983
期刊：
影响因子：
--
通讯作者：
F. Matsumura;S. M. Ghiasuddin
中科院分区：
文献类型：
--
作者：
F. Matsumura;S. M. Ghiasuddin
已获得的证据表明，环二烯类杀虫剂，例如环氧七氯和γ -六六六，模仿微毒素的作用。这些杀虫剂抑制了美洲蟑螂臀肌中GABA （γ -氨基丁酸）刺激的氯化物摄取，并直接与[3H]a-二氢微旋毒素在大鼠脑突触体中的结合竞争。此外，一些抗环二烯的昆虫菌株也对微旋毒素具有抗性。这种交叉抗性是微毒素所特有的，并不扩展到其他神经兴奋剂。这些杀虫剂，如微曲毒素，通过刺激递质释放引起中枢神经兴奋。分子结构的相似性也被指出。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微旋毒素受体相互作用所致。
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.