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1.
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   

2.
The molluscicide Frescon (N-(triphenylmethyl)morpholine) induces prolonged, irreversible contractions (contractures) in the isolated heart ventricle, penis retractor, and foot muscles of the aquatic snail Lymnaea stagnalis. It also causes contracture of the penis retractor muscle, but not the heart ventricle, of the terrestrial snail Helix aspersa. Since Frescon-induced contracture is not accompanied by a depolarization of the sarcolemma of Lymnaea heart ventricle muscle cells, it is suggested that the action of this molluscicide is associated with a membrane potential-independent activation of the contractile machinery. The rapid response of Lymnaea musculature to Frescon suggests that the direct contracture-inducing action of this molluscicide could explain its toxicity to the whole animal.  相似文献   

3.
The action of the molluscicide Frescon, which induces contractures in smooth and cross-striated muscles of the freshwater snail Lymnaea stagnalis, was compared with the action of caffeine. The results indicate that the latter agent promotes contractions in Lymnaea muscles by releasing Ca2+ from intracellular stores. Such a release could not be attributed to the action of Frescon. Furthermore, the molluscicide did not appear to alter muscle function at the level of the contractile apparatus as it did not affect the time course of caffeine-induced contractions. These results favor the hypothesis that Frescon increases sarcolemmal Ca2+ permeability.  相似文献   

4.
The molluscicide Frescon (N-(triphenylmethyl)morpholine) induces prolonged, irreversible contractions (contractures) in the isolated heart ventricle, penis retractor, and foot muscles of the aquatic snail Lymnaea stagnalis. It also causes contracture of the penis retractor muscle, but not the heart ventricle, of the terrestrial snail Helix aspersa. Since Frescon-induced contracture is not accompanied by a depolarization of the sarcolemma of Lymnaea heart ventricle muscle cells, it is suggested that the action of this molluscicide is associated with a membrane potential-independent activation of the contractile machinery. The rapid response of Lymnaea musculature to Frescon suggests that the direct contracture-inducing action of this molluscicide could explain its toxicity to the whole animal.  相似文献   

5.
The molluscicide Frescon induces irreversible contracture in smooth and cross-striated muscles of the freshwater snail Lymnaea stagnalis. This contracture can be inhibited or reversed by elevated Mg2+ and reduced Ca2+ concentrations, by the heavy metals Ni2+, Co2+, and Mn2+, by the rare earth La3+, and by the calcium channel blocker D-600. The removal of extracellular Ca2+ also prevents the expression of Frescon action. These results are consistent with the hypothesis that Frescon causes an increase in the Ca2+ permeability of the sarcolemma.  相似文献   

6.
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   

7.
The development of large complex irrigation systems presents problems of pest control which are likely to become increasingly difficult to solve by established application methods. By applying a chemical at one point in such a system use can be made of the flow of water through the system to effect the necessary distribution. This technique has been used most effectively with the molluscicide Frescon (N-tritylmorpholine). However, the complexity of many irrigation systems precludes the optimisation of the necessary rate of addition of molluscicide by any simple method. In this paper a mathematical model of an irrigation system is described which enables a detailed study of this type of application to be made with speed and economy. An analogue computer has been used to solve the equations subject to the operating conditions of the irrigation system.  相似文献   

8.
Lindane analogs, in which one or two chlorine atoms are replaced by various substituents, exhibit convulsive and lethal effects on Periplaneta americana (L.). Some analogs are as active as lindane. These effects are well related to the neuroexcitatory action which produces after-discharges in the central nervous system. Carbamate insecticides have potent convulsive and lethal effects on P. americana, which are also related to after-discharges produced in nerve cords. Convulsion caused by lindane analogs and carbamates is solely attributable to their neuroexcitatory effects on the nervous system, in spite of the difference in their ultimate modes of action.  相似文献   

9.
The hydrolysis rates, particle sizes in suspension, and the relative lipophilicity of Frescon and its analogs were determined and compared with their neurotoxic and molluscicidal effectiveness. The hydrolysis rates of these compounds were closely correlated to their neurotoxicity, and, with one exception, to their molluscicidal effectiveness as well. The aberrant behavior of the one analog could not be attributed to a retarded penetration rate or an excessively large particle size in suspension. There appears to be some, as yet, unidentified factor which determines the molluscicidal activity of this analog. However, it is likely that both neurotoxicity and molluscicidal action are the result of a nucleophilic displacement reaction, although at different targets. Also, differences in the relative molluscicidal effectiveness of the Frescon analogs at different concentrations were possibly due to variations in particle size, which appears to be a function of the type and amount of emulsifier used.  相似文献   

10.
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   

11.
Chloride ion-selective microelectrodes were used to measure the intracellular chloride activity of Lymnaea stagnalis neurons. Values ranged from 3 to 23.5 mM in different cells. Neurons with inhibitory postsynaptic potentials had significantly lower chloride activity levels than cells without such inputs. Bicarbonate-buffered saline reduced intracellular chloride levels compared with those in Hepes-buffered saline. Frescon (Shell Chemicals) produced an increase in intracellular chloride activity in 14 out of 22 neurons (mean rate of increase, 0.09 mM/min). This increase was insensitive to changes in the membrane potential: the rate of increase was reduced in bicarbonate-buffered saline. The mechanism of Frescon action is discussed in terms of a bicarbonate/chloride exchange mechanism.  相似文献   

12.
The relative potency to target and nontarget insects of ester pyrethroids and the analogous oxime ethers, and the degree of synergism of the esters with tributyl phosphorotrithioate, provide a useful guide to the importance of esterase detoxification in species specificity. These criteria indicate that esterase detoxification is a more important component of pyrethroid tolerance in Chrysopa carnea and Cryptolaemus montrouzieri larvae than in Exochomus flavipis larvae and Musca domestica adults. Studies with 3-phenoxybenzyl 2-(4-chlorophenyl)-2-cyclopropylacetate and the corresponding 2,3,4,5,6-pentafluorobenzyl ester, their oxime ether analogs, and permethrin and its thiol ester and amide analogs provide evidence that the high insecticidal activity of some ester and E-oxime ether pyrethroids, relative to that of the corresponding thiol ester and amide, is more closely associated with the dipole moment and polarizability of the central linkage and its resistance to esterase detoxification than with bond lengths or lipophilicities conferred by a specific linkage. Pentafluorobenzyl tetramethylcyclopropanecarboxylate is very effective in the vapor state for house fly control.  相似文献   

13.
The calcium entry blockers sodium nitroprusside (10?2M) and sodium pentobarbital (5 × 10?3M) had different effects on high-potassium-induced and Frescon-induced contractures in a smooth and a cross-striated muscle of the snail Lymnaea stagnalis. This suggests that Frescon causes an increase in sarcolemmal calcium permeability by a mechanism which is different from that utilized by high extracellular potassium.  相似文献   

14.
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   

15.
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   

16.
The oxons of leptophos, its desbromo analog, and its ethoxy analog all inhibit hen brain neurotoxic esterase (NTE) to a similar degree in vitro, but have large differences in minimum effective oral doses for organophosphorus-induced delayed neurotoxicity. The potencies of leptophos and ethoxyleptophos are increased 10-fold when administered to hens intravenously (iv), but the potency of desbromoleptophos is nearly the same whether administered iv or po. Leptophos distributes nearly five times more rapidly from the central compartment than does desbromoleptophos, and its attenuated oral potency may be due to slower net absorption and/or dilution by compartments other than nervous tissue. Intravenously administered phenylphosphonothionates are excreted rapidly into the gastrointestinal tract and a large proportion of the dose is eliminated in the first 48 hr. Indirect evidence indicates that ethoxyleptophos is more rapidly degraded and ethoxyleptophos-inhibited NTE recovers more rapidly than does NTE inhibited by leptophos or desbromomleptophos. It is proposed that differential aging of ethoxyleptophos chiral isomers as well as pharmacokinetic factors may contribute to the apparently anomalous behavior of these three analogs.  相似文献   

17.
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   

18.
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   

19.
The tissue distribution and excretion of [14CH3S]methamidophos was followed in female Sprague-Dawley rats after intravenous injection at a toxic, but nonlethal, dose (8 mg/kg). Radiolabel was rapidly distributed to all tissues at approximately equal concentrations. Peak tissue levels were achieved within 1–10 min except in the central and peripheral nervous system where peak levels (40 nmol/g) were found between 20 and 60 min, corresponding to peak signs of toxicity. Within 24 hr of dosing, 47% of the radioactivity was recovered in the urine and 34% as 14CO2 with <5% in the feces over 7 days. Cholinesterase (ChE) inhibition was measured in erythrocytes, plasma, and various regions of the central nervous system (CNS) at selected times after administration of methamidophos at 8 mg/kg. The degree of acetylcholinesterase (AChE) inhibition in the three CNS regions was similar, reaching a minimum of 15–20% of control values at 30–60 min, when toxicity was most severe. The degree of erythrocyte AChE inhibition was less than that of the CNS although the time course was similar. Plasma ChE inhibition was more rapid than that of the CNS or erythrocytes and reactivation was slower. When similar concentrations of methamidophos to those found in vivo were incubated with CNS homogenates, plasma, or erythrocytes in vitro (5 × 10?5M) a similar degree of inhibition occurred over the same time course. It is, therefore, concluded that the cholinergic toxicity produced by methamidophos is a result of the in vivo stability of this compound combined with its entry into the nervous system in sufficiently high concentrations to inhibit AChE.  相似文献   

20.
The binding in vitro of 14C-DDT to proteins from the hemolymph of the American cockroach was shown by means of electrophoresis and isoelectric focusing on polyacrylamide gels. The study of 14C-DDT penetration into the insect implies the hemolymph as one of the possible manners by which this insecticide could penetrate the central nervous system, and other target organs. The possibility of DDT being transported by the hemolymph bound to lipoproteins is discussed.  相似文献   

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