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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.
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
3.
A new series of 1,2,4-triazole derivatives and their corresponding carbamates have been synthesized and screened for their molluscicidal activity against two types of terrestrial snail, Helix aspersa and Theba pisana, by two methods of application, either as contact or as bran baits. Several of the tested compounds exhibited good molluscicidal activity, and T pisana was more sensitive than H aspersa. Substitution at the o- and/or p-positions of the phenyl ring with chlorine or bromine gave higher molluscicidal activity than the unsubstituted compound, with o,p-dichloro substitution being optimum. In addition, compounds containing two triazole moieties showed higher molluscicidal activity, particularly as stomach poisons, than the contact toxic effect of the corresponding compound with one triazole ring. In general, carbamate derivatives were more active than their corresponding 1,2,4-triazole derivatives. 相似文献
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5.
Makoto Kiso Masahide Nohta Keiji Tanaka Norio Kurihara Toshio Fujita Minoru Nakajima 《Pesticide biochemistry and physiology》1977,7(4):341-348
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
6.
Hydraulic erosion associated with seasonal freeze-thaw cycles is one of the most predominant factors, which drives soil stripping and transportation. In this study, indoor simulated meltwater erosion experiments were used to investigate the sorting characteristics and transport mechanism of sediment particles under different freeze-thaw conditions (unfrozen, shallow-thawed, and frozen slopes) and runoff rates (1, 2, and 4 L/min). Results showed that the order of sediment particle contents was silt>sand>clay during erosion process on unfrozen, shallow-thawed, and frozen slopes. Compared with original soils, clay and silt were lost, and sand was deposited. On unfrozen and shallow-thawed slopes, the change of runoff rate had a significant impact on the enrichment of clay, silt, and sand particles. In this study, the sediment particles transported in the form of suspension/saltation were 83.58%-86.54% on unfrozen slopes, 69.24%-84.89% on shallow-thawed slopes, and 83.75%-87.44% on frozen slopes. Moreover, sediment particles smaller than 0.027 mm were preferentially transported. On shallow-thawed slope, relative contribution percentage of suspension/saltation sediment particles gradually increased with the increase in runoff rate, and an opposite trend occurred on unfrozen and frozen slopes. At the same runoff rate, freeze-thaw process had a significant impact on the relative contribution percentage of sediment particle transport via suspension/saltation and rolling during erosion process. The research results provide an improved transport mechanism under freeze-thaw condition for steep loessal slopes. 相似文献
7.
Tariq A. Andrea David D. Stranz Alex Yang Daniel A. Kleier Kanu M. Patel James E. Powell Thomas P. Price Dennis S. Marynick 《Pest management science》1990,28(1):49-68
Dimethyl 2-methyl-5-(chloropyridin-2-yl)pyrrole-3,4-dicarboxylates in which the chlorine atom is substituted at different positions of the pyridine ring have widely varying biological properties. The 3-chloro analog (I) is a post-emergence and pre-emergence herbicide, the 4- and 5-chloro analogs (II, III) are post-emergence herbicides but not pre-emergence, and the 6-chloro analog (IV) is inactive. Computer graphic and molecular mechanics analyses of their molecular conformations showed that the 4- and 5-chloro analogs adopt a coplanar, intramolecularly hydrogen bonded conformation whereas the 3-chloro analog does not. High-level quantum mechanical calculations of the conformational preferences of related model systems were in agreement with these results. Based on this, II and III were predicted to have higher octanol/water partition coefficients relative to I, leading to higher soil binding and weaker xylem transport, hence their observed weaker pre-emergence activities. Experimental measurements of octanol/water partition coefficients, soil binding, and infrared hydrogen bonding studies verified these predictions. Molecular modeling techniques are usually used for designing compounds to fit enzyme active sites and designing putative receptor models. This study demonstrates the usefulness of these techniques for dealing with transport problems. 相似文献
8.
The comparative ester hydrolysis and selective toxicity of carbamate insecticides were studied in four mammalian species. Hydrolysis rates of carbaryl and ethiofencarb (Croneton) were examined in the rat, mouse, guinea pig, and gerbil. Respiratory 14CO2 resulting from the hydrolysis of orally administered [carbonyl-14C]carbamates (0.2 mg/kg) was taken as measure of in vivo hydrolytic capabilities. Ester hydrolysis was found to be greater for ethiofencarb than for carbaryl in all species tested, although the relative order of hydrolysis among species was the same with both compounds. After 24 hr, gerbils had hydrolyzed 91% of the ethiofencarb and 65% of the carbaryl. Guinea pigs hydrolyzed somewhat less of the compounds, 65 and 58%, but considerably more than rats and mice, about 40 and 25%. Comparing hydrolysis capabilities to acute toxicity data revealed that those species exhibiting the greatest hydrolysis were equally or more susceptible to carbamate poisoning than those having lesser hydrolytic capabilities. While ester hydrolysis destroys the anticholinesterase activity of carbamates, it is clear from these findings that factors other than hydrolysis are largely responsible for the variation in toxicity of the carbamates to different mammalian species. 相似文献
9.
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
10.
砂磨机制备铜基营养保护剂悬浮剂的工艺优化 总被引：2，自引：0，他引：2
为提高铜基营养保护剂悬浮剂的悬浮率和稳定性,通过正交实验和单因素实验方法,从浆料质量分数、研磨转速、研磨介质与浆料质量比及研磨时间4个因素出发,研究了通过砂磨机制备铜基营养保护剂悬浮剂的优化工艺。结果表明:研磨转速对制剂粒径影响最大;研磨介质与浆料质量比对制剂分散颗粒比表面积影响最大;浆料质量分数对粒径和比表面积的影响均最小。其最佳制备工艺条件为:浆料质量分数60%,研磨转速1 500 r/min,m(研磨介质):m(浆料)=1.5:1,研磨时间80 min。在此条件下,所得铜基营养保护剂悬浮剂的悬浮率均大于90%,且其分散性、水质适应性和水温实验均符合相关标准要求。研究结果可为铜基营养保护剂的开发应用提供理论基础及工艺参考。 相似文献
11.
Paul F. Luckham 《Pest management science》1989,25(1):25-34
The word stability is ubiquitous in colloid science but means different things to different people. In a suspension concentrate it is possible to identify three different physical processes which may lead to instability in a particulate system, namely a change in particle size due to Ostwald ripening, particle aggregation and particle sedimentation. Although these processes may occur simultaneously they are here treated separately in order to promote understanding of the physical forces involved. 相似文献
12.
The present work was carried out to evaluate, the molluscicidal activity of cold water, boiled water, methanol, ethanol, acetone and chloroform extracts of some plant species against Biomphalaria alexandrina snails. Preliminary screening tests on 10 plant species showed that the highest molluscicidal potency was recorded for Euphorbia splendens, Atriplex stylosa and Guayacum officinalis. Exposure of B. alexandrina snails to plant’s methanol extracts led to a significant reduction in their survival and growth rates. In addition, newly hatched snails were susceptible to plant’s methanol extracts than elder ones. LC25 of methanol extract from these plants caused a considerable reduction in the infectivity of Schistosoma mansoni miracidia to the snails. It caused a reduction in number of cercariae per snail during the patent period and in the period of cercarial shedding. The results, also, revealed that the glucose concentration in treated snails was increased in haemolymph, while soft tissue glycogen decreased. The activities of glycogen phosphorylase, succinate dehydrogenase (SDH), glucose-6-phosphatase and acetylcholinesterase (AchE) in homogenate of snail’s tissues were reduced (P < 0.001) in response to treatment with plants methanol extract, while glucose-6-phosphate dehydrogenase (G-6-PD) activity increased (P < 0.001). It was concluded that the application of LC25 of methanol extracts of E. splendens, A. stylosa and G. officinalis may be helpful in snail control as it interferes with the snails’ biology and physiology. 相似文献
13.
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
14.
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
15.
Chau H. Wu Jozef van den Bercken Toshio Narahashi 《Pesticide biochemistry and physiology》1975,5(2):142-149
The effects of 14 DDT analogs on the resting and action potentials of the crayfish giant axon were investigated using the intracellular microelectrode technique. These analogs can be classified into three groups, excitatory, blocking, and dualist. An excitatory analog tends to increase the excitability of the axonal membrane, and has hydrophobic side chains on the para positions whose optimal size equals that of the ethoxy group. A blocking analog suppresses the action potential without affecting the resting potential, and has hydrophilic side chains capable of forming hydrogen bonds. A dualist has both excitatory and blocking actions, and the latter may be related to restriction in rotation imposed by the grouping on the benzylic carbon. However, the dividing lines between these categories are not sharp, the compounds tending to fall along a spectrum between pure excitatory and pure blocking activity. 相似文献
16.
A series of 2-amino-5-substituted pyridine derivatives was synthesized and their molluscicidal activity against white garden, Theba pisana (Müller), and brown garden, Helix aspersa (Müller), snails was investigated by two methods of application. Some of these compounds showed strong activity under laboratory conditions against the two types of snail. T pisana was more sensitive to the tested compounds than H aspersa. The most effective compounds were 2-amino-5-(benzotriazole-1-ylmethyl)-3-methylpyridine, 2-amino-5-[1-(benzotriazole-1-yl)nonyl]-3-methylpyridine and 2-[(1,2,4-triazole-1-ylmethyl)amino]-3-methylpyridine which exhibited high molluscicidal activity. The toxicity results are discussed in relation to the chemical structures. © 1999 Society of Chemical Industry 相似文献
17.
Larry G. Hansen Elizabeth M. Cozzi Robert L. Metcalf Terry K. Hansen 《Pesticide biochemistry and physiology》1985,24(1):136-148
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
18.
银锭夜蛾Macdunnoughia crassisigna Warren是豆类作物和十字花科蔬菜上重要的食叶性害虫。因其具有暴食性，迁飞性等特点，逐渐成为东北、华北地区重要的农业害虫。由于缺乏有效的绿色防控技术，目前化学农药仍是防控银锭夜蛾有效的方法之一。为提高银锭夜蛾的防治效果，以银锭夜蛾性信息素主要成分顺-7-十二碳烯乙酸酯（Z7-12：Ac）、顺-9-十四碳烯乙酸酯（Z9-14：Ac）为母体结构，通过酯化反应得到结构新颖的类似物14个，结构经GC-MS、1H NMR、13C NMR和HR-MS确证。触角电生理试验（EAG）表明，有11个类似物具有较好的EAG反应。EAG抑制试验发现，类似物4、13和14具有明显的抑制效果。在100 μg剂量下，类似物4对Z7-12：Ac的抑制率达50.2%。风洞试验表明，当添加1500 μg的类似物4时，对银锭夜蛾的干扰尤为显著，没有成虫到达诱芯。田间试验表明，类似物4具有潜在的抑制活性，当添加150、1500 μg的类似物4时，平均诱捕量与性信息素存在显著性差异，抑制率分别为56.90%、59.34%。研究结果有助于揭示性信息素拮抗剂对银锭夜蛾种内化学通讯调控方式，为银锭夜蛾绿色防控技术提供新的思路与手段。 相似文献
19.
采用界面聚合法制备了以聚脲树脂为囊材的15%高效氯氟氰菊酯微囊悬浮剂。在制备过程中,以油相质量与初次用水质量相比得到初次油水比,探究了不同初次油水比对高效氯氟氰菊酯微囊悬浮剂理化性质的影响。设定4个不同初次油水比 (Ri) 处理,分别为Ri = 1 : 0.55、1 : 0.69、1 : 0.83和1 : 0.97,通过光学显微镜、扫描电镜、激光粒度分布仪对所制备微囊的形貌进行表征,并测定包覆率与贮藏稳定性。结果显示:当Ri分别为1 : 0.83和1 : 0.97时,所制备的15%高效氯氟氰菊酯微囊悬浮剂成囊质量高,微囊形貌好,微囊包覆率90%以上,粒径3~4 μm (D95),贮存稳定性合格。本研究可为制备高效氯氟氰菊酯微囊悬浮剂提供参考。 相似文献
20.
Substitution of silicon for carbon was explored in etofenprox and MTI-800, primarily to establish the suitability of silicon for pesticide construction and to probe steric effects. It was shown that silicon is an effective building block for insecticides with subtle qualitative and quantitative differences relative to the carbon analogs. The silanes were slightly less toxic to insects than the carbon analogs (relative potency of 0.2-0.6) but the silane analog of MTI-800 was considerably less toxic to fish (0% mortality at ≥50 mg liter?1) than MTI-800 itself (LC50 = 3 mg liter?1). The mode of action of both carbon and silicon compounds was similar in the intact, electrode-implanted cockroach and involved repetitive firing of a sensory nerve; potency measurements were also made using an in-vitro nerve assay. The possible metabolic and physicochemical contributions to the observed insecticide potencies were explored using synergism studies, physical chemistry measurements and quantum mechanical calculations. 相似文献