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1.
The pesticides, chlordimeform and amitraz, and their metabolites, demethylchlordimeform, N1-(2,4-dimethylphenyl)-N-methylformamidine, and 2,4-dimethylformanilide, are effective at concentrations as low as 3 μM in raising the firing rate of endogenously active neurosecretory fibres in the isolated neurohaemal organs of Carausius morosus. Molecules such as bunamidine and cetrimide, with cationic detergent properties, produced sporadic bursting which did not elevate the overall firing rate to any great extent. Indeed, bunamidine could induce complete block of action potentials at concentrations as low as 30 μM. The local anesthetics, procaine, lidocaine, and benzocaine, do not induce block of activity at least up to a level of 1 mM. They have no effect at concentrations lower than 100 μM. Between 100 μM and 1 mM lidocaine and benzocaine produce a small increase in firing rate. Procaine produced a pronounced increase in the frequency of firing. The phenolic amines, octopamine, synephrine, and tyramine, markedly increased electrical activity. The catecholamines, dopamine, noradrenaline, and adrenaline, by contrast, only produced a weak excitation. Neither α- nor β-adrenergic blocking agents were effective in antagonizing the electrical activity induced by chlordimeform or phenolic amines until relatively high concentrations of about 1 mM were used. Chlordimeform was able to induce high-frequency bursts from sense organs associated with the epidermis and body-wall musculature in larvae of Musca domestica and Calliphora erythocephala. Octopamine did not induce any similar bursting activity in these sense organs. These results are discussed in relationship to current views on the mode of action of the N-aryl amidines. It is concluded that the excitatory effects of these compounds upon neurohaemal organs and sense organs are more likely to result from a direct action upon voltage sensitive channels of the nerve membranes, rather than by an effect mediated by interactions with octopamine receptors.  相似文献   

2.
Application of phosphorothionate and phosphorothiolothionate insecticides at micromolar concentrations inhibited the hindgut contraction of Periplaneta americana induced by proctolin or proctodeal nerve stimulation. At identical concentrations, oxon analogues of these insecticides had no effect on proctolin or neural responses in the hindgut while a phosphonate insecticide, EPN, had a long-lasting potentiating action on contraction. The present investigation identifies a new site of organophosphorus insecticide action that may be a useful model system for the design and testing of pesticides that interfere with peptidergic transmission.  相似文献   

3.
The joint action of insecticides, or of mixtures of insect growth regulators and insecticides, on the susceptible (S) strain and diflubenzuron-resistant (Rd) strain of the cotton leafworm Spodoptera littoralis Boisd. was investigated. The joint action of the insecticides and/or insect growth regulator mixtures was determined by mixing them in proportion to their activity equivalents at the LD25 or ED25 levels. A total of 15 mixtures of two synthetic pyrethroids, two organophosphorus, one carbamate and one organochlorine insecticides, were applied to the fourth-instar larvae of the S and Rd strains. The insecticide mixtures cypermethrin/methomyl and cypermethrin/endrin exhibited high and moderate levels of synergism on the S strain, respectively. However the mixtures chlorpyrifos/methomyl, phosfolan/methomyl, and phosfolan/endrin produced antagonism, while the other mixtures showed varying levels of additive effects. The response of the fourth-instar larvae of the S strain, to the joint action of diflubenzuron/juvenoid, diflubenzuron/insecticide, or insecticide/juvenoid mixtures, revealed that diflubenzuron produced high levels of synergism when combined with methoprene and progressively less with fenvalerate, methomyl and cypermethrin. On the other hand, the mixture diflubenzuron/triprene was antagonistic. Fenvalerate with the two juvenoids produced synergism while methomyl showed an additive effect with methoprene. However, the mixtures cypermethrin/methoprene, cypermethrin/triprene and methomyl/triprene produced antagonism. The mixtures that produced potentiation on the fourth-instar larvae of the S strain lost their high potency when tested against the Rd strain. The results also indicated that insecticide/juvenoid mixtures, when applied on 2-day-old pupae of the S strain, were synergistic, except in the case of cypermethrin/methoprene and methomyl/triprene mixtures, for which additive effects were observed. When the mixtures that had synergistic effects on the S strain were tested on the Rd strain, the results revealed that their synergistic effects were apparently reduced. This was attributed to the fact that the generalised levels of tolerance in the Rd strain towards various compounds may have influenced the several defence mechanisms to act against the synergistic action of the chemical mixtures.  相似文献   

4.
Sodium channel blocker insecticides (SCBIs) are a relatively new class of insecticides, with a mechanism of action different from those of other classes of insecticides that target voltage-gated sodium channels. These compounds have no effect at hyperpolarized membrane potentials, but cause a voltage-dependent, nearly irreversible block as the membrane potential is depolarized. The mechanism of action of SCBIs is similar to that of local anesthetics (LAs), class I anticonvulsants and class I antiarrhythmics. In this article, we review the physiological actions of these compounds on the whole animal, the nervous system and sodium channels, and also present the results from recent studies that elucidate the receptor site of SCBIs.  相似文献   

5.
The distribution of pyrethroids in insects has been studied using a combination of mathematical modelling and experimental observation. This approach has resulted in the formulation of a physiological model of the pharmaco-kinetics of cypermethrin applied topically to larvae of Spodoptera littoralis. Development of this model from simpler two- and three-compartment models is described. Simple models, whilst capable of complex behaviour, consider only the average rates and magnitudes of pharmaco-kinetic processes over whole animals, and cannot account for differences in concentration of insecticide between individual tissues. This can be achieved by using physiological models, but these require more experimental information for their validation. Moreover, unless simplifying assumptions are made, analytical solutions are not feasible for the large number of equations necessary to define such models. The modelling studies prompted an investigation of (1) in-vivo binding of insecticide to insect tissues, (2) the sizes of body compartments, and (3) the factors which affect the distribution of toxicant between these compartments. Binding has a marked effect on pharmacokinetic profiles and may result in oscillatory behaviour. During poisoning, the total bound cypermethrin increases proportionally to the cube root of the elapsed time. This results in a rapid rate of increase over early elapsed times (< 3h) which slows to approach a more linear form thereafter. Average sizes for the body compartments of larvae of Spodoptera littoralis Boisd, and the steady-state distribution of cypermethrin in these compartments are described. Although the haemolymph, which acts as the main distributive phase during poisoning, forms the largest compartment by volume, it has a low affinity for cypermethrin and distribution reaches steady state within 5 min after topical application. The nerve cord (the target tissue), which is the smallest compartment, has the highest steady-state concentration of cypermethrin. The distribution of cypermethrin in larval tissues is related to the ratios of tissue dry matter to water content.  相似文献   

6.
The metabolism in vivo and in vitro of [14C]parathion and [14C]paraoxon was studied in a susceptible (LS) and an organophosphorus-resistant (Q) strain of the sheep blowfly, Lucilia cuprina. Both strains detoxified the insecticides in vivo via a number of pathways, but the resistant strain produced more of the metabolites diethyl phosphate and diethyl phosphorothionate. No difference was found between strains in the rate of penetration of the compounds used. Also, in vitro studies showed no difference between strains in the sensitivity of head acetylcholinesterase to inhibition by paraoxon. Both the microsomal and the 100,000g supernatant fractions degraded paraoxon, but resistance in Q could be explained by the eightfold greater rate of diethyl phosphate production with or without added NADPH. Parathion was also degraded to diethyl phosphorothionate by an NADPH-requiring enzyme in microsomal preparations from both strains. However, Q produced significantly more diethyl phosphorothionate in vivo than LS. It was concluded that organophosphorus resistance in Q was due mainly to a microsomal phosphatase hydrolyzing phosphate but not phosphorothionate esters, probably enhanced by a microsomal oxidase detoxifying the latter.  相似文献   

7.
Schistocerca poisoned with insecticides may lose more than 30% of their body weight and 60% of their hemolymph volume within 24 hr. In spite of this and the impairment of the nervous system, poisoned Schistocerca show a remarkable ability to control the osmotic concentration and ionic composition of the remaining hemolymph. Much of the water loss from poisoned locusts can be attributed to evaporation through the spiracles, due to the progressive failure of the animal to close the spiracular valves. Another significant factor is a massive transport of fluid across the gut wall into the fore and midgut. This fluid may be regurgitated causing a further loss in weight.  相似文献   

8.
五种常用杀虫剂对灰飞虱繁殖力的影响   总被引:5,自引:0,他引:5  
为合理使用杀虫剂防治灰飞虱,采用稻茎浸渍法测定杀虫剂氟虫腈、吡虫啉、毒死蜱、三唑磷和高效氯氟氰菊酯对灰飞虱3龄若虫的室内活性,并用LC50、LC75和LC,90测定灰飞虱的繁殖力.结果表明,经氟虫腈和吡虫啉处理的3龄若虫和成虫,所产的第2代若虫数均少于清水对照;而经毒死蜱、三唑磷和高效氯氟氰菊酯处理的3龄若虫和成虫,所产的第2代若虫数均多于对照,其中经高效氯氟氰菊酯LC50处理的3龄若虫所产的第2代若虫数最多,比对照多53.3%,极显著高于对照.在尼龙网隔离的水泥池内稻麦套作,接灰飞虱成虫后分别用氟虫腈39.9 mL/667m2和吡虫啉53.2mL/667m2处理,第2年的虫量仅为对照的33.5%和64.6%;而用毒死蜱59.9mL/667m2、三唑磷98.6mL/667 m2以及高效氯氟氰菊酯99.8mL/667m2处理,第2年的虫量分别比对照多1.73、1.35和1.93倍.  相似文献   

9.
不同药剂对山楂叶螨的亚致死效应   总被引:2,自引:1,他引:2  
在室内采用叶碟饲养的方法,利用生命表技术研究了四螨嗪、阿维菌素、甲氰菊酯及三唑锡对山楂叶螨的亚致死效应.结果表明,在成虫期,LC10、LC25剂量的阿维菌素、甲氰菊酯及三唑锡可使成螨的产卵量显著降低,除甲氰菊酯LC10外,其余处理可使次代种群的内禀增长率(rm)由0.173降低至0.133~0.167;在若螨Ⅰ期,LC10、LC25剂量的阿维菌素可使rm由0.237降低至0.197~0.199;甲氰菊酯LC10对雌螨的产卵有明显的刺激作用,rm由0.237提高到0.259,而LC25则无明显影响;在卵期,四螨嗪LC10对rm无明显影响,但LC50、LC25可使rm由0.173降低至0.149~0.154.  相似文献   

10.
The ovicidal action of four insecticides and three insect growth regulators, on eggs of various ages of the susceptible (S) strain of Spodoptera littoralis, was investigated. The results revealed that diflubenzuron was the most toxic compound tested on 0-1-day-old eggs, followed by triprene and then methoprene; chlorpyrifos came next in its toxicity, followed by cypermethrin then fenvalerate; methomyl was the least effective. With the progress of embryonic development, 1-2-day-old eggs showed slight tolerance to the action of the pesticides and juvenoids, but apparently resisted the action of diflubenzuron. Eggs 2-3 days old showed increased tolerance to the insecticides and diflubenzuron and, to a lesser extent, to the action of the two juvenoids. A total of 21 insecticide or insect growth regulator-insecticide mixtures, based on their toxicity equivalents (LD25 + LD25), were applied jointly on 0-1-day-old eggs of the S strain. The mixtures which produced high synergism on this stage could be arranged, according to their decreasing order of potentiation, as follows: fenvalerate/diflubenzuron, cypermethrin/triprene, methomyl/methoprene, cypermethrin/methoprene, fenvalerate/ methoprene, cypermethrin/methomyl, cypermethrin/diflubenzuron, fenvalerate/triprene, diflubenzuron/methoprene and methomyl/triprene. The mixtures that produced synergistic effects on 0-1-day-old eggs were also tested against the 1-2 and 2-3-day-oldeggs of the S strain. Theresults indicated that themixtures fenvalerate/diflubenzuron, and cypermethrin with either triprene or diflubenzuron, when tested on 1-2-day-old eggs, produced levels of synergism nearly similar to those achieved on newly deposited eggs. On the other hand, the mixtures cypermethrin/methomyl, and fenvalerate with methoprene or triprene, showed comparatively lower levels of synergism. However, the synergistic action of the mixture cypermethrin/methoprene, previously detected on newly deposited eggs, became an additive effect on 1-2-day-old eggs. Only the mixtures fenvalerate/diflubenzuron, cypermethrin/triprene and fenvalerate/methoprene showed synergism on 2-3-day-old eggs. The mixtures which showed synergistic effects on 0-1-day-old eggs of the S strain were further tested on eggs of various ages of the diflubenzuron-resistant (Rd) strain. As regards 0-1-day-old eggs, only the combinations cypermethrin/triprene, methomyl/methoprene and fenvalerate/methoprene produced additive effects. The mixture cypermethrin/diflubenzuron was still synergistic against newly deposited eggs of the Rd strain, in a manner similar to that indicated with the S strain. Apparent levels of antagonism were shown to the other insecticide-juvenoid mixtures as well as to the diflubenzuron/methoprene combination. The combinations cypermethrin/methomyl and fenvalerate/diflubenzuron had some effect on the freshly deposited eggs of the Rd strain but produced lower levels of potentiation. With the increase in age of the eggs, the mixture cypermethrin/diflubenzuron showed a lower level of synergism on the 1-2 day-old eggs than was observed in younger eggs. The additive effects, previously detected with some of the mixtures on newly deposited eggs became an antagonistic effect for the 1-2-day-old eggs. The eggs at this stage were more able to resist thejoint action of the other mixtures tested. Moreover, with further increase in the age of the eggs, the combination cypermethrin/diflubenzuron produced a lower level of potentiation on 2-3 day-old eggs, followed by fenvalerate/diflubenzuron at an even lower level, while the other mixtures showed various levels of antagonism.  相似文献   

11.
The effects of pyrethroids on the on-going electrical activity of the axons of neurosecretory cells from the brain of fifth instar Rhodnius prolixus have been studied using extracellular electrodes. Low concentrations of the pyrethroids decamethrin, bioresmethrin, permethrin, and bioallethrin all produce dramatic increases in the overall frequency and dramatic changes in the pattern of electrical activity when applied directly to the exposed brain and corpora cardiaca in an otherwise intact insect. This change in activity was brought about by a recruitment in active units and the production of phasic acivity. A doubling of frequency over that of controls was brought about by low doses of the pyrethroids, namely decamethrin, 1 × 10?10M; bioresmethrin, 2 × 10?10M; permethrin, 1 × 10?9M; and bioallethrin, 2 × 10?7M. Similar hyperactivity of this system occurred during intoxication of intact insects following topical application of LD95 bioresmethrin. The enhanced sensitivity shown by neurosecretory cells over that of other cell types is discussed, as is the possibility that the increases in electrical activity of neurosecretory axons may result in massive neurohormonal release and thereby contribute to the eventual poisoning of the insect.  相似文献   

12.
杀虫剂对昆虫的亚致死效应的研究进展   总被引:13,自引:0,他引:13  
杀虫剂亚致死效应是农药生态毒理学研究的一个重要方面.根据近年文献资料,综述了杀虫剂对昆虫生殖力、发育历期、行为和抗药性方面的亚致死效应,阐述了有关解毒酶的作用机制.杀虫剂亚致死效应对农业生态系统具有深远的影响,应展开更加深入、全面的研究.  相似文献   

13.
A ligature round the “waist” of the housefly was shown to block effectively the flow of haemolymph between the abdomen and the rest of the body, but it did not prevent the toxic action of certain contact insecticides. These included representatives of four major chemical types. The ligature appeared to have little effect on the speed of action of these compounds, suggesting that the haemolymph is not important in their transport to the site of action.  相似文献   

14.
The actions of pyrethroid insecticides were tested on isolated giant axons of the cockroach Periplaneta americana, using oil-gap, single-fibre recording techniques. Current-clamp and voltage-clamp experiments were used to determine the actions of pyrethroids on axonal membrane potentials and ionic currents. Treatment with deltamethrin at micromolar concentrations caused gradual depolarisation of the axon accompanied by a reduction in amplitude of the action potential. This depolarisation was enhanced by an increase in stimulation frequency. Other synthetic pyrethroids: 3,4,5,6-tetrahydrophthalimidomethyl (1RS)-cis-3-[(RS)-2,2-dimethylcyclopropyl]-2,2-dimethylcyclopropanecarboxylate, biopermethrin and its (1S)-enantiomer, (1R)-tetramethrin, S-bioallethrin, bioresmethrin and its (1S)-enantiomer, cismethrin, and 5-benzyl-3-furylmethyl (E)-(1R)-cis-2,2-dimethyl-3-(2-oxothiolan-3-ylidenemethyl)cyclopropanecarboxylate (RU-15525, ‘Kadethrin’) were investigated. The (1S)-enantiomers were inactive, but all the other pyrethroids tested, apart from deltamethrin, induced prolonged negative (depolarising) after-potentials. All the treatments with the active pyrethroids resulted in the appearance of a voltage and time-dependent ‘maintained’ sodium conductance. The duration of this ‘slow’ conductance varied considerably depending on the pyrethroid under test. Clearly, the effectiveness of pyrethroids on whole insects is not determined only by the degree to which they directly modify the properties of sodium channels. Nevertheless, voltage-clamp experiments on isolated axons readily permit direct comparison of the actions of different pyrethroids on the sodium channels of insect neurones.  相似文献   

15.
The ultrastructure of the neurosecretory cells of the corpora cardiaca (CC) of Locusta migratoria and Rhodnius prolixus was altered following incubation of the isolated glands in 1 μM bioresmethrin. The insecticide induced formation of large vacuoles in the soma and extensive exocytosis in the axon terminals of treated cells. Pretreatment of the CC with 1 μM tetrodotoxin blocked the action of bioresmethrin. Bioresmethrin affected the distribution and shape of mitochondria in neurosecretory cells. In Rhodnius, numerous mitochondria were found clustered in vacuoles in neurosecretory cells of the CC treated with bioresmethrin. Some of these mitochondria were abnormally elongated while others showed signs of fission. The results are discussed in relation to the action of bioresmethrin on neurosecretory cells.  相似文献   

16.
Nereistoxin suppressed the excitatory actions of α- and γ-BHC and HEOD in the central nervous system of Periplaneta americana (L.). However, it did not affect the neurotoxic action of DDT and DBrDT. Since nereistoxin is an acetylcholine antagonist, it is postulated that BHC and HEOD act to produce high level of acetylcholine and the resulting after-discharges, while DDT and DBrDT seem to attack the noncholinergic region of insect nervous system.  相似文献   

17.
Application of the formamidine pesticides chlordimeform (CDM) and desmethylchlordimeform (DCDM) induced the release of hyperlipemic hormone from the isolated corpus cardiacum (CC) of the locust, Locusta migratoria. Pretreatment of locusts with reserpine (10 μg/locust) had no effect on formamidine-induced release of the hyperlipemic hormone. The action of CDM and DCDM on isolated CC was blocked by the α-adrenergic-receptor blocker, phenoxybenzamine, but not by the β-adrenergic blocker, propranolol. These formamidines also potentiated the release of the hyperlipemic hormone induced by electrical stimulation of nervus corpus cardiacum II (NCC II). The evidence presented in this paper indicates that, in locusts, CDM and DCDM, or their metabolites, act on postsynaptic aminergic (octopamine) receptors in the glandular lobe of the CC, inducing the release of hyperlipemic hormone.  相似文献   

18.
Little information is available on the actions of β-carboline convulsants on insect GABA receptors or their potential as insecticides. Accordingly, two compounds (3-ethoxy-β-carboline, 3-EBC; dimethoxy-β-carboline-3-methyl ester, DMCM) were studied for their effects on Drosophila melanogaster larval neuron discharge and also in lethality bioassays on adult female D. melanogaster and adult male Blattella germanica. Recordings of nerve spiking in the isolated larval central nervous system showed that 3-EBC and DMCM inhibited nerve discharge, and this inhibitory effect was not additive with that of GABA, confirming that the inhibition was expressed through an action on the GABA receptor. Nerve blockage induced by β-carbolines could not be reversed by picrotoxinin, indicating that there may exist some overlap or negative allosteric coupling between the picrotoxinin and β-carboline binding sites. DMCM and 3-EBC effectively antagonized the effects of exogenously applied GABA in nerve preparations from insecticide-susceptible larvae. In contrast, preparations from the rdl strain of D. melanogaster, which possesses a GABA receptor that is highly resistant to cyclodienes and related convulsants, were less sensitive to the GABA antagonist effect of DMCM. Neither of the β-carbolines produced any appreciable mortality in insects, even when synergized with piperonyl butoxide or S,S,S-tributyl phosphorotrithioate, The toxicity of the β-carbolines is probably limited by their relatively weak effects on the GABA receptor and perhaps also by pharmacokinetic factors. These considerations, coupled with the cross-resistance observed in cyclodiene-resistant insects, suggest that the currently available β-carbolines are not viable as lead compounds for insecticide screening efforts. © 1997 SCI.  相似文献   

19.
An investigation was made of the action of the juvenile hormone analogues (JHAs) methoprene (ZR-515) and 3-[5-(4-ethylphenoxy)-3-methylpent-3-enyl]-2, 2-dimethyloxirane (R-20458), and the insecticides chlorpyrifos and methomyl, when applied, separately or in combination, to the late insect stages of susceptible (S) and aminocarb-resistant (Rm) strains of Spodoptera littoralis Boisd. Sixth-instar larvae of the Rm strain showed detectable levels of cross-resistance to chlorpyrifos, methomyl and R-20458. However, cross-resistance to methoprene was less pronounced in the Rm strain. Treatment of the same instar with the ED50 of methoprene produced an appreciable level of sterility in the S strain, but this level decreased in the Rm strain. Similar treatment with R-20458 caused a lower level of sterility in the S strain and the Rm strain was less affected. In the S strain, the ED25 of either chlorpyrifos or methomyl when applied simultaneously with the ED25 of R-20458, produced an antagonistic effect and the Rm strain was more capable of resisting the joint action of these compounds. The treatment, ED25 chlorpyrifos + ED25 methoprene produced an additive effect on the S strain, while the Rm strain tolerated their combined action. Nevertheless, the treatment, ED25 methomyl + ED25 methoprene produced additive effects on both the S and Rm strains. The prepupae of the Rm strain tolerated the action of the insecticides methomyl and chlorpyrifos. A similar pattern of cross-resistance was also detected against the action of the two hormones at the ED25 level, while at the ED25 level, both the S and Rm strains were almost equally sensitive to the action of the two juvenoids. Chlorpyrifos-JHA combinations produced additive effects on prepupae of the S strain while the Rm strain completely resisted their joint action. Methomyl-JHA combinations produced high potentiation in the S strain, but the Rm strain remained insensitive to their joint action. Detectable levels of tolerance to the action of chlorpyrifos and methomyl at the ED25 and ED50 levels were indicated in 2-day-old pupae of the Rm strain. This was less evident in the case of JHAs, particularly methoprene, which was to some extent equally effective on both strains; the reproductive ability of the S and Rm strains was highly affected by this compound. The pupae of the Rm strains were equally as affected as those of the S strain by the combination ED25 chlorpyrifos+ ED25 R-20458. Nevertheless, the two strains showed antagonism to the action of chlorpyrifos with methoprene. A high level of potentiation was produced in the S strain to the combination of methomyl and R-20458 but the Rm strain was able to withstand their combined action. Of interest in this respect was the action of the combination of methomyl and methoprene, for which high levels of potentiation were detected in pupae of the S and Rm strains. This combination also Produced a high percentage of sterility in mated females of the Rm strain.  相似文献   

20.
甲酸乙酯对三种主要仓储害虫的熏蒸作用   总被引:1,自引:0,他引:1  
为明确甲酸乙酯对仓储害虫的实际控制效果,避免二氧化碳对熏蒸作用的影响,该研究利用循环熏蒸系统(FTFS),测定甲酸乙酯对米象、赤拟谷盗、谷蠹三种主要仓储害虫混合虫态的熏蒸作用.结果表明:在25℃、70%RH条件下,甲酸乙酯43.34、80.72、99.08、117.74、146.49mg/L 熏蒸处理6 h,对赤拟谷盗和谷蠹混合虫态有很好的控制作用,死亡率大于95.96%;甲酸乙酯80.72、99.08、117.74、146.49mg/L处理对米象混合虫态的杀虫效果较好.甲酸乙酯对米象蛹的杀虫效果较差.  相似文献   

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