2 CLASSES OF PYRETHROID ACTION IN THE COCKROACH
2 CLASSES OF PYRETHROID ACTION IN THE COCKROACH
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DOI：
10.1016/0048-3575(81)90084-5
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发表时间：
1981-01-01
影响因子：
4.7
通讯作者：
CASIDA, JE
中科院分区：
文献类型：
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作者：
GAMMON, DW;BROWN, MA;CASIDA, JE
拟除虫菊酯根据其对体内和体外记录的颈感觉神经的影响以及在给药的美洲斑蠊（P. americana）中产生的症状分为2类（I型和II型）。I类化合物包括除虫菊酯、s -生物丙烯菊酯、[1R，顺式]氯甲菊酯、氯菊酯的1R、反式和1R、顺式异构体、吩菊酯和氯菊酯，以及肟o -苯氧苄醚。给药个体的电生理记录显示了颈感觉尖峰序列，有时也显示了来自颈运动神经和中枢神经系统的尖峰序列。在体外实验中，低浓度的拟除虫菊酯可在单次电刺激后诱发颈感觉神经的重复放电。这种体外测量，用于评估结构-活性关系的标准化，表明只有1R，杀虫异构体是高效的神经毒素。对离体神经最有效的化合物是[1R，反式]-和[1R，顺式]氯菊酯，每一种活性为3。10-13 M. I型化合物的中毒症状是坐立不安、不协调、多动、虚弱和瘫痪。II型化合物包括[1R，顺式，α。[S]-和[1R，trans,.alpha]。氯氰菊酯、溴氰菊酯和氰戊菊酯。这些.alpha。-氰苯氧苄酯拟除虫菊酯在体内或体外均不会引起颈感觉神经的重复放电；它们会引起不同的症状，包括明显的抽搐期。另外两种含有。的拟除虫菊酯。-氰基取代基，即甲氰菊酯和肟O-。根据它们对颈感觉神经的作用，这些化合物被归类为I型，但这些化合物的症状类似于II型。本文讨论了拟除虫菊酯类杀虫剂对蟑螂明显的两类作用，以及它们在其他生物中的神经生理作用和症状。
Pyrethroids are divided into 2 classes (Types I and II) based on their effects on the cercal sensory nerves recorded in vivo and in vitro and on the symptomology they produce in dosed cockroaches, P. americana. Type I compounds include pyrethrins, S-bioallethrin, [1R,cis]resmethrin, kadethrin, the 1R,trans and 1R,cis isomers of tetramethrin, phenothrin and permethrin, and an oxime O-phenoxybenzyl ether. Electrophysiological recordings from dosed individuals reveal trains of cercal sensory spikes and sometimes also spike trains from the cercal motor nerves and in the CNS. Low concentrations of these pyrethroids act in vitro to induce repetitive firing in a cercal sensory nerve following a single electrical stimulus. This in vitro measurement, standardized for evaluating structure-activity relationships, shows that only 1R, insecticidal isomers are highly effective neurotoxins. The most potent compounds on the isolated nerve are [1R,trans]- and [1R,cis]tetramethrin, each active at 3 .times. 10-13 M. The poisoning symptoms of Type I compounds are restlessness, incoordination, hyperactivity, prostration and paralysis. Type II compounds include [1R,cis,.alpha.S]- and [1R,trans,.alpha.S]cypermethrin, deltamethrin and [S,S]fenvalerate. These .alpha.-cyanophenoxybenzyl pyrethroids do not induce repetitive firing in the cercal sensory nerves either in vivo or in vitro; they cause different symptoms, including a pronounced convulsive phase. Two other pyrethroids with an .alpha.-cyano substituent, i.e., fenpropathrin and an oxime O-.alpha.-cyanophenoxybenzyl ether, are classified as Type I based on their action on a cercal sensory nerve but the symptoms with these compounds resemble Type II. The 2 classes of pyrethroid action evident with the cockroach are discussed relative to their neurophysiological effects and symptomology in other organisms.