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1.
The neuroexciting activity of DDT and its analogs to produce repetitive responses on the nerve cord of Periplaneta americana was determined using the extracellular electrode method. The convulsive activity on P. americana and the insecticidal effect on Callosobruchus chinensis were also examined. It was found that the convulsive and insecticidal activities increase almost proportionally with increase in the neuroexciting activity within a set of p,p′-substituted DDT analogs. The intimate connections among these biological effects suggest that symptoms such as convulsion and death caused by DDT analogs are closely related with their neuroexcitory effect and there is a common mode of action in spite of differences in insect species.  相似文献   

2.
The effects of lindane on carbohydrate and lipid reserves of Periplaneta americana were studied in adult male insects. Topical application of lindane resulted in depleted levels of glycogen in the fat body (90% depletion) and thoracic musculature (57% depletion) and a 55% decrease in hemolymph trehalose (anthrone-positive material) by the prostration stage of poisoning. By contrast, lindane caused a 42% elevation of fat-body acylglycerol reserves and an associated 60% decrease of hemolymph free fatty acid levels. The lindane effects on carbohydrate and lipid were expressed also in head-ligated insects, thereby indicating that the results are not attributable solely to the action of lindane on the corpus cardiacum. The results are discussed in light of the proposal that lindane, and some other insecticides, cause indiscriminate release of neuroactive factors from the neuroendocrine system and that the consequent perturbation of physiological balance may contribute to the lethal action of the insecticide.  相似文献   

3.
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   

4.
Hexadeuterio-lindane(γ-BHC-d6) was several times as toxic as lindane against the mosquito (Culex pipiens pallens), house fly (Musca domestica), German cockroach (Blattella germanica) and American cockroach (Periplaneta americana). The neuroexcitatory activity of these two compounds did not differ. Lindane was considerably synergized by piperonyl butoxide, but lindane-d6 was not. A large isotope effect was observed in the in vivo breakdown of lindane-d6. Thus, the intrinsic toxicities of both compounds are equivalent. The difference in insecticidal activity seems to be due to the different rates of detoxifying biodegradation caused by the kinetic deuterium isotope effect.  相似文献   

5.
Knockdown and lethal activities of meta- and para-substituted benzyl (1R)-trans-chrysanthemates against the house fly were measured under synergistic conditions using piperonyl butoxide as an inhibitor of oxidative metabolism and NIA 16388 as an inhibitor of hydrolytic degradation. The variations in these activities were quantitatively analyzed in terms of physicochemical substituent effects using electronic, hydrophobic, and steric parameters of the aromatic substituents, and regression analysis. The most significant parameter in determining these activities is the steric bulkiness represented by the van der Waals voluem, the effect of which is highly specific to substituent positions. The substituent effects on knockdown and lethal activities against the house fly are shown to correspond well, respectively, with those on the convulsive and lethal activities against the American cockroach. The relationship between these symptomatic activities against the house fly and the neurophysiological activities determined by using excised nerve cords from American cockroaches were also quantitatively analyzed. Each house fly symptomatic activity was found to be analyzable by a linear combination of the neuroexcitatory and neuroblocking activity indices when the transport factor was separated by using the hydrophobicity parameter.  相似文献   

6.
A number of substituted benzyl (1R)-trans-chrysanthemates and related compounds were synthesized. Their symptomatic activities in terms of levels which induce convulsions as well as cause death in American cockroaches were determined by injection with and without application of synergists as inhibitors of metabolism. The neuroexcitatory and neuroblocking activities were also determined in terms of minimum effective concentrations to induce repetitive train of impulses and conduction blockage, respectively, to central nerve cords excised from the cockroaches and immersed in Ringer's solution. Correlations between symptomatic and neurophysiological activities were analyzed quantitatively with the aid of molecular hydrophobicity parameter and regression analysis. Each symptomatic activity from which the effect of metabolism is eliminated was found to be analyzable by means of a linear combination of indices for two types of neurophysiological activity when the transport factor is separated by using the hydrophobicity parameter. A closer correlation was found between neuroblocking activity and the “convulsive” effect than between neuroexcitatory activity and the “convulsive” effect, whereas both neurophysiological effects operate together on the cockroaches resulting in paralysis and death.  相似文献   

7.
The effects of chlordimeform and lindane on levels of 5-hydroxytryptamine, tryptophan, and N-acetyl dopamine were studied in the cerebral ganglia of the american cockroach, Periplaneta americana. The effects of chlordimeform on nerve cord levels of 5-hydroxytryptamine, tryptophan, dopamine, and octopamine, and the effect of lindane on cerebral ganglia levels of dopamine were also investigated in this species. Topical applications of chlordimeform deplete 5-hydroxytryptamine and tryptophan from the cerebral ganglia whereas levels of n-acetyl dopamine are elevated. The effect of chlordimeform on these compounds is dose-dependent. Similar chlordimeform-induced effects are observed in the nerve cord, and octopamine levels are also depleted in this tissue following treatment with chlordimeform. A biphasic response to chlordimeform is observed in the nerve cord for dopamine levels with a 40% decrease evident after 2 hr and a 30% increase apparent after 6 hr. In contrast to chlordimeform, lindane does not affect 5-hydroxytryptamine and tryptophan levels in the cebral ganglion but low doses of this insecticide effect increases in brain levels of dopamine and n-acetyl dopamine.  相似文献   

8.
Biodegradability of lindane analogs using house fly whole body, microsomes, and microsome supernatant fraction was examined. It decreased in the order of alkoxy ～ methylthio > methyl analogs > lindane in the whole body experiments, as well as with microsomes in the presence of NADPH. With the supernatant in the presence of glutathione, a different trend was observed. The synergistic effects of piperonyl butoxide when used together with lindane analogs were mostly explained in terms of the inhibition of the microsomal metabolism. Piperonyl butoxide was also shown to inhibit the penetration of compounds into the fly body and to make the central nervous system of the American cockroach less sensitive to the action of insecticides causing after and repetitive discharges. It was observed that the value of the percentage of metabolic disappearance of insecticides after a certain period decreases as the dose level initially applied in the whole body experiments increases. The synergistic ratio parallels the percentage of disappearance value after the insecticidal activity test period when a dose corresponding to the unsynergized LD50 is initially applied. When quantitative comparisons are required for biodegradability of insecticides using house flies as the test insects, it should be on the basis of direct metabolism experiments using a fixed dose throughout the series of insecticides, but not on the basis of the synergistic ratio.  相似文献   

9.
Although the molluscicide Frescon is a strong neurotoxin to the Lymnaea stagnalis central nervous system in vitro, it is probable that the exposure of the whole animal to this molluscicide fails to result in central nervous system abnormalities: Frescon does not appear to reach the brain in sufficient quantity to disrupt its normal activity. However, only those Frescon analogs found to be neurotoxic were molluscicidal, suggesting some related mode, if not site, of action. Frescon and its analogs may act by affecting excitable tissues other than the nervous system (e.g., the snail musculature) by altering certain functional and/or structural membrane properties.  相似文献   

10.
The effects of p,p′-DDT and four of its analogs on electrical activity in the central nervous system of the cockroach, Periplaneta americana (L.), were investigated. Cockroaches were injected intraabdominally with an organochlorine compound at LD50 96-hr doses (except for p,p′-DDE). Extracellular recordings were made from the central nervous system at 1 hr, 24 hr, or 3 weeks postinjection. p,p′-DDT, methoxychlor, and p,p′-DDD induced behavioral changes (tremors, jitters, hyperexcitability) and repetitive firing in the central nervous system prior to 1 hr postinjection. By 24 hr postinjection, most behavioral signs of poisoning had disappeared, though repetitive firing could still be readily elicited in the central nervous system. Cockroaches injected with o,p′-DDT, however, usually required about 48 hr before overt signs of poisoning became apparent. Cockroaches treated with p,p′-DDT or o,p′-DDT behaved normally at 3 weeks postinjection but still displayed a significant occurrence of repetitive firing in the central nervous system. A mechanism is proposed to explain how a cockroach might recover behaviorally from a sublethal dose of an organochlorine compound but still display repetitive firing in its central nervous system. A direct “cause and effect” relationship between repetitive firing in the central nervous system and mortality (and external signs of poisoning) is therefore questioned.  相似文献   

11.
Dihydrooxadiazines are structural analogs of octopamine and were compared with octopamine for their ability to compete with [3H]dihydroergocryptine ([3H]DHE) for binding sites on DHE-sensitive receptors, to stimulate adenylate cyclase activity in nervous system homogenates of Periplaneta americana L., and to modulate the action of the peptide proctolin on the oviducal muscles of Locusta migratoria L. [3H]DHE binding was inhibited by low concentrations (μM range) of octopamine, phentolamine, N-demethylchlordimeform (DCDM) and several dihydrooxadiazines. The tested dihydrooxadiazines acted as aminergic agonists in stimulating cyclic AMP production in cockroach nervous system homogenates and did not show additive effects with octopamine, whereas additivity was observed with 5-hydroxytryptamine. The relative potency of octopaminergic antagonists, including mianserin, cyproheptadine, phentolamine, and gramine, to block octopamine-mediated elevation of cyclic AMP production was similar to the rank-order potency of the same antagonists to inhibit dihydrooxadiazine-mediated elevation of cyclic AMP production. Octopamine, 2-(4-bromophenyl)-5,6-dihydro-4H-1,3,4-oxadiazine (4-Br-PDHO), and 8-Br-cyclic AMP caused increased phosphorylation of proteins that are phosphorylated by exogenously added cyclic AMP-dependent protein kinase. These results indicate that the dihydrooxadiazine-induced rise in cyclic AMP levels in homogenates of the cockroach nervous system results directly in activation of an endogenous cyclic AMP-dependent protein kinase. 4-Br-PDHO behaved similarly to octopamine in modulating the action of proctolin-induced contractions in locust oviducal muscles. These observations suggest that dihydrooxadiazines act as octopamine agonists and have an octopaminergic action in modulating the action of proctolin. Thus, it is proposed that dihydrooxadiazines exert at least part of their insecticidal and miticidal actions through interaction with the octopaminergic system.  相似文献   

12.
The effect of chlordimeform and 18 related compounds on the aggregation behavior of the negatively geotactic larvae of the cattle tick, Boophilus microplus was investigated. Aggregations were treated and hyperactivity in the forms of immediate dispersal, delayed dispersal, and prolonged leg waving evaluated. A marked structure-activity relationship with delayed dispersal resulted; most active were the N-monomethyl formamidines, N′-(2,4-dimethylphenyl)-N-methylformamidine and demethylchlordimeform. Other compounds, including chlordimeform, with structures compatible with metabolism to N-monomethyl formamidines were also active. Delayed dispersal caused by those possessing the N,N-dimethyl moiety was antagonized after inhibition of oxidative N-demethylation to N-monomethyl analogs by piperonyl butoxide. Since the N-monomethyl moiety had already been reported as important in the killing action of the formamidines in cattle tick larvae, the possibility of a relationship between delayed dispersal and acaricidal effectiveness was examined and percentage mortality at 24 hr found to correlate positively with the rate of onset of dispersal.Delayed dispersal was not characteristic of the responses to other acaricides such as lindane, allethrin, carbaryl, and coumaphos. In addition, the monoamine oxidase inhibitors, tranylcypromine, pargyline, and nialamide, did not induce delayed dispersal and showed no lethal effects.  相似文献   

13.
The effect of DDT, 11 analogs, dieldrin, and lindane was studied on the pressure-area curves obtained by compressing monolayers of lecithin. The minimum cross-sectional area of lecithin and the compounds was measured by photography of models. All compounds shifted the pressure area curves in a direction and to an amount that suggested they formed 1:1 complexes with lecithin, and the complex had the cross-sectional area of the compound. DDT did not complex with cholesterol monolayers. Both DDT and DDMU formed complexes with phospholipids from Torpedo electroplax which resembled those with lecithin. The lack of difference in effects on monolayers between physiologically active and inactive analogs indicated that the monolayer effects did not explain the physiological action of DDT.  相似文献   

14.
The factors which cause lindane resistance in the Third Yumenoshima strain, a strain of house flies highly resistant to insecticides, were studied using hexadeuterated lindane. Hexadeuterated lindane has the same physicochemical properties as lindane, but the former is much less biodegradable than the latter. The LD50 ratio of lindane to hexadeuterated lindane in this strain, deuterium isotope effect on LD50 values, was larger than that in SNAIDM, a susceptible (nonresistant) strain. The penetration rates of labeled and nonlabeled lindane through the insect cuticle were about the same for both strains. Thus, penetration rate does not cause resistance. The metabolic degradation of lindane in the resistant strain in vivo occurred much faster than in the susceptible strain. This was also the case for lindane degradation processes in vitro such as microsomal oxidation and glutathione conjugation. In both strains, significant isotope effects were observed in the degradation rates in vitro of labeled and nonlabeled lindane. Therefore, principal biodegradation and detoxication pathways should include reactions which cleave the CH bonds. When the much less biodegradable d6 counterpart of lindane was applied to both strains, the susceptible strain became much more highly intoxicated than the other within 20 to 30 min. This indicates that a combination of both greater degradability and probably lower sensitivity at the action site are the main factors underlying resistance in the Third Yumenoshima strain.  相似文献   

15.
The insecticidal activity of lindane analogs, in which some chlorine atoms were replaced by other groups susceptible to microsomal oxidative metabolism, was determined against mosquitos, house flies, and German cockroaches. When tested with a synergist, piperonyl butoxide, one of the methylthio analogs was as active as lindane, whereas several others were also highly active. By examining the ratio of synergized and unsynergized LD50 values (synergistic ratio value), the highly insecticidal methylthio, methoxy, and methyl analogs appear to undergo metabolic detoxication effectively in house flies. By means of in vitro metabolism experiments using microsomal fraction from house fly abdomen, the methoxy, ethoxy, and methylthio analogs were shown to be metabolized rapidly at similar rates. The synergized insecticidal activities of these compounds against various insect species relate linearly with each other, suggesting that the oxidative degradation is inhibited by the synergist to a similar extent and that the transport process to the site of action is not a limiting factor in determining the relative insecticidal activity.  相似文献   

16.
Frescon (N-triphenylmethyl morpholine) is a strong neurotoxic agent when applied to the in vitro brain of Lymnaea stagnalis. Ten Frescon analogs were tested in order to determine their degree of neurotoxicity. Nine of the ten analogs were found to be neurotoxic to a greater or lesser degree. Triphenylmethanol (a hydrolysis product of Frescon), however, did not exhibit neurotoxicity. These results form part of an investigation to determine the plausibility of the snail central nervous system being a target for Frescon action.  相似文献   

17.
Preseizure and seizure EEG patterns elicited by the pyrethroid insecticides, deltamethrin and cis-permethrin, were compared in immobilized Sprague-Dawley rats. Deltamethrin (1–3 mg/kg, iv) produced a preseizure EEG pattern of high-amplitude, slow, 2- to 5-Hz synchronized cortical waves or spike-wave complexes. cis-Permethrin (20–40 mg/kg, iv) elicited an immediate EEG change characterized by 6- to 12-Hz high-amplitude waves with intermingled high-voltage spikes. DDT (50–70 mg/kg, iv) produced a sustained EEG activation similar to that seen after cis-permethrin, but of higher frequency. All three insecticides produced generalized EEG seizure activity, but this was more prominently associated with poisoning due to deltamethrin. cis-Permethrin and DDT gave rise to EEG seizures only at lethal doses. Electrodes stereotaxically positioned in ventral hippocampus, caudate, putamen, thalamus, septum, red nucleus, and cerebellum detected no preferential activation of any of these subcortical sites in either preconvulsive or convulsive phases of poisoning. These results indicate that both deltamethrin and cis-permethrin can have marked effects on mammalian EEG activity. This does not support the hypothesis of differing sites of action, i.e., peripheral vs. central, for the two types of compound. The more pronounced seizure-inducing action of deltamethrin may instead reflect a greater efficacy of cyanopyrethroids at target sites within the central nervous system.  相似文献   

18.
The action of avermectin was studied in the leg muscle and the central nervous system of the American cockroach, Periplanata americana L. Avermectin at a low concentration (10?7M) causes a failure of the leg muscles to respond to external stimuli within 30 min without affecting the magnitude of contraction. Avermectin was found to stimulate Cl? uptake by the leg muscles within 4 min at 10?7M. The threshold concentration to cause such stimulation was on the order of 10?8M. This stimulatory action could be antagonized by picrotoxinin (10?4M) and to a lesser extent by bicuculline methiodide (10?4M). The phenomenon is observable under both Na+-free and K+-free conditions. It was concluded that the action of avermectin is to open the chloride channel on the plasma membrane. This action of avermectin does not seem to be mediated through GABA, GABA receptors, diazepine receptors, or picrotoxinin receptor in this insect species, and therefore suggests that avermectin directly attacks the chloride channel proper both in the central nervous and the neuromuscular systems.  相似文献   

19.
Solutions of tetramethrin, RU 11679, or cismethrin caused uncoupled convulsions in 30–40 min in exposed thoracic ganglia from SNAIDM house flies at concentrations down to 10?10M: whereas these same compounds at 10?6M concentrations failed to produce poisoning symptoms when perfused onto the exposed ganglia of the kdr strain of house fly. The pyrethroid analogs examined had a negative temperature coefficient of action on the exposed thoracic ganglia from SNAIDM flies. DDT and GH-74 possessed positive temperature coefficients of action on the exposed thoracic ganglion of susceptible house flies. It is concluded that the central nervous system of the kdr strain of house fly is resistant to pyrethroid action; furthermore, the resistance appears to be widespread throughout the house fly nervous system, involving sensory, motor, and central neural elements.  相似文献   

20.
Pyrethroids are divided into two 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, Periplaneta 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 × 10?13M. The poisoning symptoms of Type I compounds are restlessness, incoordination, hyperactivity, prostration, and paralysis. Type II compounds include [1R,cis,αS]- and [1R,trans,αS]cypermethrin, deltamethrin, and [S,S]fenvalerate. These α-cyanophenoxybenzyl pyrethroids do not induce repetitive firing in the cercal sensory nerves either in vivo or in vitro; moreover, they cause different symptoms, including a pronounced convulsive phase. Two other pyrethroids with an α-cyano substituent, i.e., fenpropathrin and an oxime O-α-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 two classes of pyrethroid action evident with the cockroach are discussed relative to their neurophysiological effects and symptomology in other organisms.  相似文献   

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