Flannigan S A, Tucker S B, Key M M, Ross C E, Fairchild E J, Grimes B A, Harrist R B
Br J Ind Med. 1985 Jun;42(6):363-72. doi: 10.1136/oem.42.6.363.
Synthetic pyrethroids are lipophilic insecticides whose biological activity seems to be directly related to their chemical structure. In this investigation differences in cutaneous sensation were detected by human participants between synthetic pyrethroids with a cyano group in the (S)-configuration of the 3-phenoxybenzyl alcohol of their molecular structure (fenvalerate) and those that do not (permethrin). A strong relation was noted between insecticidal potency and degree of induced cutaneous sensation for the alpha-cyano and non-cyano pyrethroids, with a prominent difference between the two. No sensation was observed by any of the same participants on topical exposure to the inert ingredients of these agents. A linear correlation between concentration and degree of induced dysaethesia was observed for both pyrethroids. Regressing the cutaneous sensation on the common logarithm of concentration resulted in a regression equation of Y = 84.0 + 31.0X1 for fenvalerate and Y = 27.5 + 15.8X1 for permethrin. A highly efficacious therapeutic agent for pyrethroid exposure was noted to be dl-alpha tocopherol acetate. An impressive degree of inhibition of paraesthesia resulted from the topical application of vitamin E acetate, with a therapeutic index of almost 100%.
合成拟除虫菊酯是亲脂性杀虫剂，其生物活性似乎与其化学结构直接相关。在本研究中，人类受试者检测到分子结构中3-苯氧基苄醇的（S）-构型带有氰基的合成拟除虫菊酯（氰戊菊酯）与不带氰基的合成拟除虫菊酯（氯菊酯）之间存在皮肤感觉差异。对于α-氰基和非氰基拟除虫菊酯，观察到杀虫效力与诱发皮肤感觉程度之间存在很强的相关性，两者之间存在显著差异。相同的受试者在局部接触这些药剂的惰性成分时均未观察到感觉。两种拟除虫菊酯均观察到浓度与诱发感觉异常程度之间存在线性相关性。将皮肤感觉与浓度的常用对数进行回归分析，氰戊菊酯得到的回归方程为Y = 84.0 + 31.0X1，氯菊酯为Y = 27.5 + 15.8X1。已注意到dl-α生育酚醋酸酯是一种用于拟除虫菊酯接触的高效治疗剂。局部应用维生素E醋酸酯可显著抑制感觉异常，治疗指数几乎达100%。
