Quantitative structure-activity studies of substituted benzyl chrysanthemates: 9. Calcium uptake inhibition in crayfish nerve cord and lobster axon homogenates in vitro by sunthetic pyrethroids

Twenty-five synthetic pyrethroids and related chemicals were assessed for their effects on the uptake of Ca²⁺ (as ⁴⁵Ca²⁺) by crude homogenates prepared from crayfish (Procambarus clarkii) nerve cords and 20 were assessed on the uptake by homogenates prepared from lobster (Panulirus japonicus) axons. A parabolic relationship was demonstrated between inhibition of Ca²⁺ uptake for this series of chemicals and lipophilicity (log P) in both species when tested at 5 μM. Optimal log P for maximal inhibition was located at about 6.6 and 84(±6)% inhibition was obtained with resmethrin. Compounds of higher or lower log P were either weaker inhibitors, not inhibitors or occasionally resulted in slightly increased levels of Ca²⁺ uptake. No direct correlations between the potential for the pyrethroids to inhibit Ca²⁺ uptake and the potential for these agents to increase the frequency of spontaneous discharges in crayfish nerve cords, to induce repetitive firing in American cockroaches, or the lethality to cockroaches or to any other neurophysiological or toxicity parameter could be established. It was concluded that although some synthetic pyrethroids are moderately potent inhibitors of Ca²⁺ uptake into nerve cord and axonic preparations (i.e., I₅₀ for trans-resmethrin equals 1 μM) this inhibition alone does not relate to the neurophysiological changes in isolated nerve preparations or to the toxicity of these agents in insects.     

Inhibition by decamethrin and resmethrin of hormone release from the isolated rat neurohypophysis—A model mammalian neurosecretory system

The isolated rat neurophypophysis, which shows a calcium-dependent hormone release when depolarized in vitro was used as a model system to investigate the effects of the pyrethroids decamethrin and resmethrin on mammalian nervous tissue. Both compounds inhibited neurohypophysial hormone release in response to electrical stimulation, decamethrin being more potent than resmethrin. Decamethrin reduced the hormone content of the neurohypophysis. Resmethrin did not reduce stored hormone significantly and its effects on release were dose dependent. They could be mimicked by raising the [Na⁺] of the medium but not by lowering the [Ca²⁺]. Resmethrin had no effect on the release of hormone following depolarization of the tissue with a raised [K⁺]. The results are consistent with the suggestion that the compounds do not act on the potential-dependent secretion process but rather on the mechanism linking depolarization of the secretory terminals with the arrival of action potentials possibly by interfering with sodium-channel activation and inactivation.     

DDT inhibition of Ca-ATPase of the peripheral nerves of the American lobster

A Ca-ATPase highly sensitive to DDT has been found in peripheral nerves of lobster, Homarus americanus. The observed I₅₀ for this Ca-ATPase toward DDT is on the order of 10^?9M and has a low temperature quotien. The ATPase seems to work over a wide range of ATP concentrations. It is stimulated by Ca²⁺ (optimum 0.1 mM) and shows sensitivity to Na⁺ (optimum 20 mM) and K⁺ (optimum 20 mM) ions. The fact that it is highly sensitive to ruthenium red (I₅₀ = 10 μM) suggests that the enzyme is a Ca-ATPase and not a Mg-ATPase. Furthermore the enzyme is not a CaMg-ATPase, since the presence of Mg²⁺ along with Ca²⁺ ion is not required for its activity. DDT is found to inhibit the process of Ca²⁺ binding in the axonic membrane only in the presence of ATP. The evidence suggests the important role of the Ca-ATPase in regulating Ca²⁺ concentrations in the membrane. The possible significance of DDT inhibition of the ATPase is discussed.     

Binary mixtures of pyrethroids produce differential effects on Ca influx and glutamate release at isolated presynaptic nerve terminals from rat brain

Isolated rat brain synaptosomes were used to evaluate the action of pyrethroid mixtures on Ca²⁺ influx and subsequent glutamate release under depolarizing conditions. In equipotent binary mixtures at their respective and/or estimated EC₅₀s with deltamethrin always as one of the two components, cismethrin, λ-cyhalothrin, cypermethrin, esfenvalerate and permethrin were additive and S-bioallethrin, fenpropathrin and tefluthrin were less-than-additive on Ca²⁺ influx. In binary mixtures with deltamethrin always as one of the two components, esfenvalerate, permethrin and tefluthrin were additive and λ-cyhalothrin was less-than-additive on glutamate release. Binary mixture of S-bioallethrin and cismethrin was additive for both Ca²⁺ influx and glutamate release. Only a subset of pyrethroids (S-bioallethrin, cismethrin, cypermethrin, and fenpropathrin) in binary mixtures with deltamethrin caused a more-than-additive effect on glutamate release. These binary mixtures were, however, only additive (cismethrin and cypermethrin) or less-than-additive (S-bioallethrin and fenpropathrin) on Ca²⁺ influx. Therefore, increased glutamate release evoked by this subset of pyrethroids in binary mixture with deltamethrin is not entirely occurring by Ca²⁺-dependent mechanisms via their action at voltage-sensitive calcium channels. These results suggest that pyrethroids do not share a common mode of toxicity at presynaptic nerve terminals from rat brain and appear to affect multiple target sites, including voltage-sensitive calcium, chloride and sodium channels.     

不同灌水处理对滨海盐碱地土壤阳离子组成及玉米干物质累积的影响

采用田间试验对不同灌水处理灌水后玉米地（天津滨海盐碱地）0~60 cm土层土壤K⁺/Na⁺、Ca²⁺/Na⁺及玉米干物质累积量进行研究,共设计4个处理,分别为LI₁₀（常规滴灌,灌水10 mm）、LI₂₀（常规滴灌,灌水20 mm）、FI₁₀（膜下滴灌,灌水10 mm）和FI₂₀（膜下滴灌,灌水20 mm）。结果表明：灌水后不同灌水方式下灌水量较大的处理0~60 cm各土层K⁺/Na⁺均大于灌水量较小的处理,且均表现出0~20 cm土层K⁺/Na⁺较大,40~60 cm土层K⁺/Na⁺较小;相同灌水量下膜下滴灌处理0~60 cm各土层Ca²⁺/Na⁺均较大,灌水后不同灌水处理0~60 cm各土层Ca²⁺/Na⁺差异较小,变化范围为0.10~0.22;FI₂₀处理0~20 cm土层K⁺/Na⁺和Ca²⁺/Na⁺大于其他处理,分别达到0.78和0.22;随着灌水次数的增多,LI₂₀和FI₁₀处理0~20 cm土层K⁺/Na⁺和Ca²⁺/Na⁺均逐渐增大,LI₁₀处理则均逐渐减小;灌水后各处理之间0~60 cm各土层K⁺/Na⁺和Ca²⁺/Na⁺差异均达显著水平;全生育期干物质累积量与其对应的0~20 cm土层（K⁺/Na⁺）/Ca²⁺二次拟合相关系数均达0.90以上,相同（K⁺/Na⁺）/Ca²⁺下,FI₂₀处理干物质累积量始终最大,LI₁₀处理始终最小;（K⁺/Na⁺）/Ca²⁺>1.72时,各处理干物质累积量均随（K⁺/Na⁺）/Ca²⁺的增大而增大。     

Influence of calmodulin and ATP on DDT inhibition of Na/Ca exchange in the axolemma-rich nerve preparation from the American lobster

The effects of DDT on the Na/Ca exchange system were studied by using an axolemma-rich nerve membrane preparation from walking legs of Homerus americanus, the American lobster. The Na/Ca exchange system was measured by using two criteria: Na⁺ stimulated ⁴⁵Ca²⁺ uptake by the membrane vesicles and Na⁺Ca²⁺ protein kinase-phosphatase (formally called Ca-ATPase) as measured by the production of ³²P-labeled inorganic phosphate from [γ-³²P]ATP in the presence of Na⁺ and Ca²⁺. Activities of both systems were stimulated by the addition of exogenous calmodulin. DDT's inhibitory actions on both systems were reduced when an excess of calmodulin was added. Also addition of large amounts of ATP (or γ-thio-ATP) to the former system had an effect to reduce levels of DDT inhibition. DDT appears to act on the protein kinase proper as well as calmodulin itself in this system in a reversible manner.     

Pyrethroid insecticides: Potent,stereospecific enhancers of mouse brain sodium channel activation

Deltamethrin and NRDC 157, pyrethroid insecticides that produce different poisoning syndromes in mammals, enhanced veratridine-dependent, sodium channel-mediated ²²Na⁺ uptake in mouse brain synaptosomes. Concentrations producing half-maximal enhancement were 2.5 × 10^?8M (deltamethrin) and 2.2 × 10^?7M (NRDC 157). This effect was stereospecific: The nontoxic 1S enantiomers had no significant effect on veratridine-dependent activation. At high deltamethrin concentrations, enhancement was maximal at 5 × 10^?5?1 × 10^?4M veratridine. Pyrethroid enhancement was completely blocked by 5 × 10^?6M tetrodotoxin, and neither pyrethroid affected ²²Na⁺ uptake in the absence of veratridine at concentrations up to 1 × 10^?5M. The relative potencies of deltamethrin and NRDC 157 in the synaptosomal sodium channel assay agree well with their relative acute toxicities to mice when administered by intracerebral injection. These findings demonstrate that pyrethroids exemplifying both characteristic poisoning syndromes are potent, stereospecific modifiers of sodium channel function in mammalian brain.     

Characterization of 11 commercial pyrethroids on the functional attributes of rat brain synaptosomes

The action of 11 commercial pyrethroids on Ca²⁺ influx and glutamate release was assessed using high-throughput functional assays with rat brain synaptosomes to better understand the mechanistic nature of pyrethroid-induced neurotoxicity and aid in the reassessment of pyrethroids in vivo. Concentration-dependent response curves for each of the non-cyano and α-cyano containing pyrethroids were determined and the data used in a cluster analysis. The previously characterized α-cyano pyrethroids that induce the CS-syndrome (cypermethrin, deltamethrin, and esfenvalerate) increased Ca²⁺ influx and glutamate release, and clustered with two other α-cyano pyrethroids (β-cyfluthrin and λ-cyhalothrin) that shared these same actions. Previously characterized T-syndrome pyrethroids (bioallethrin, cismethrin, and fenpropathrin) did not share these actions and clustered with two other non-cyano pyrethroids (tefluthrin and bifenthrin) that likewise did not elicit these actions. Our current findings indicate that pyrethroids that have an α-cyano group (with the exception of fenpropathrin) were more potent enhancers of Ca²⁺ influx and glutamate release under depolarizing conditions than pyrethroids that did not possess this functional group. The collective data set does not support the hypothesis that pyrethroids, as a class, act in a similar fashion at presynaptic nerve terminals.     

3种盐胁迫对玉米幼苗生长及叶片抗氧化酶和离子累积的影响

选取2个玉米品种(金玉819和金单999),探讨了3种盐胁迫(NaCl、Na_2SO_4和NaNO_3)对玉米幼苗生长、抗氧化酶活性以及叶片中K~+、Na~+、Ca~(2+)累积的影响。结果表明:3种不同类型的盐胁迫均会导致玉米幼苗鲜重下降,地上部鲜重金玉819下降超过28.6%,金单999下降超过18%;盐胁迫下金玉819叶片SOD酶活上升2.1倍以上, POD酶活性最高上升4.5倍,APX最高上升2.1倍,CAT最高上升2.2倍;金单999叶片SOD酶活最高上升2.1倍,APX最高上升1.6倍,CAT最高上升1.9倍。2个基因型玉米胁迫下叶片内Na~+含量上升4.5～6.3倍;NaCl和NaNO_3处理下,K~+/Na~+比对照降低90%～93%,而Na_2SO_4处理下K~+/Na~+下降78%～82%,金玉819和金单999的Ca~(2+)/Na~+比对照分别降低了85%～90%和92%～94%。综合分析表明NO~-_3引起的次生盐害对玉米生产危害较大。与金单999相比,金玉819对盐胁迫更加敏感,相同Na~+浓度处理下,金玉819的鲜重和SOD酶活性下降显著且拥有较低的K~+/Na~+和Ca~(2+)/Na~+值。     

微咸水离子组成对膜下滴灌土壤孔隙结构的影响

为探讨不同阳离子组成微咸水灌溉对膜下土壤孔隙结构的影响,开展2a田间定位试验,设置当地地下水灌溉（CK）、NaCl微咸水灌溉（T1）、KCl微咸水灌溉（T2）、CaCl₂微咸水灌溉（T3）、MgCl₂微咸水灌溉（T4）5个处理,利用CT扫描技术研究不同阳离子组成微咸水对土壤孔隙结构的影响。结果表明：与CK处理相比,随灌水次数增多,添加Na⁺处理的土壤大孔隙度显著降低,添加K⁺、Ca²⁺、Mg²⁺处理的土壤大孔隙度显著增加,2022年添加Na⁺处理的大孔隙度平均降低了44.49%,添加K⁺、Ca²⁺、Mg²⁺处理的土壤大孔隙度平均分别增加了5.73%、80.73%、25.75%;在2021—2022年期间,与CK相比,4种不同阳离子处理土壤孔隙成圆率均呈增加趋势,其中添加Ca²⁺、Mg²⁺处理增加显著,土壤孔隙成圆率平均增加区间分别为25.52%~30.94%、17.46%~23.19%;连续灌溉2a之后,添加Na⁺和K⁺处理的土壤开裂程度加重,土壤稳定性变差,而添加Ca²⁺和Mg²⁺对改善土壤结构、提高土壤入渗性能作用明显。     

Effects of glyphosate on uptake,translocation, and intracellular localization of metal cations in soybean (Glycine max) seedlings

Root-fed or foliar-applied glyphosate [N-(phosphonomethyl) glycine] reduced uptake and translocation of Ca²⁺ and Mg²⁺, but not K⁺, by soybean [Glycine max (L.) Merr. “Hill”] seedlings as measured by atomic absorption spectrometry. Histochemical techniques revealed that cells of secondary roots that were formed after glyphosate treatment were deficient in Ca²⁺. The relative distribution of Ca²⁺ in control root and leaf cells was mitochondria > plastids > cytoplasm. Glyphosate severely reduced Ca²⁺ content and eliminated intracellular concentration of Ca²⁺ in the mitochondria of both root and leaf cells. Glyphosate had no effects on K⁺ distribution at the ultrastructural level. These results support the view that glyphosate effects on distribution of divalent metal cations may be related directly or indirectly to the phytotoxicity of the herbicide.     

The effects of pyrethroids on the electrical activity of neurosecretory cells from the brain of Rhodnius prolixus

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.     

Gibberellin influence on membrane disruption by thiocarbamate herbicides

Vernolate (0, 8, 16, 31, 62, 125.0, or 250.0 ppbw) incorporated into sand inhibited the growth of wheat (Triticum aestivum L. cv Holley) at 125.0 ppbw. These growth inhibition and morphological responses were virtually identical to wheat response to EPTC at 125 ppbw. ¹⁴C from vernolate (carbonyl labeled) (125.0 ppbw) was absorbed into wheat seedlings at approximately 1.8 μM on the presumption that the ¹⁴C present was [¹⁴C]vernolate. Since the response of wheat to the thiocarbamate herbicides resembles a gibberellic acid (GA) deficiency and cell enlargement requires the presence of functional plasmalemmas and tonoplasts, the question of membrane disruption by excessive concentrations of thiocarbamate herbicides and potential reversal thereof by GA₃ was studied by measuring the efflux of K⁺, Na⁺, and Mg²⁺. GA₃ (0.003 μM) stimulated lettuce leaf disc growth in diameter and fresh weight. This GA-stimulated increase in size and weight was reversed by 1 mM EPTC. Betacyanin efflux from beet leaf tonoplasts was increased by 1 mM EPTC and this efflux was not reversed by exogenous GA₃ (0.3 μM). This influence by supraoptimal EPTC concentrations was shown to be via membrane disruption, which obviated any possible GA influence by eliminating the functionality of the membranes requisite to the development of a GA response. It is concluded that viable mode-of-action studies must measure physiological responses consistent with the symptomology of herbicide responses normally observed with each herbicide at field concentrations.     

DDT and pyrethroids: Receptor binding and mode of action in the house fly

The mode of action of DDT and pyrethroids was investigated in the house fly, Musca domestica L, using drug:receptor binding techniques. Both in vivo and in vitro binding studies demonstrated the existence of membrane receptors which bind specifically to [¹⁴C]DDT and [¹⁴C]cis-permethrin. The receptors show properties to be expected of a critical target site of these insecticides. These include negative temperature correlation with binding, relatively nonsensitivity to DDE, and sensitivity to Ca²⁺. The receptor sites are readily saturated at 45–90 nM [¹⁴C]DDT and have an apparent disassociation constant (K_d) of 12.2 nM. The maximum number of binding sites was estimated to be 17 pmol DDT/mg membrane protein (0.34 pmol/house fly head). Competition studies showed DDT, cis-permethrin, and cypermethrin bind to the same receptor but not at precisely the same site. The addition of Ca²⁺ to the incubation buffer significantly inhibited the binding of both [¹⁴C]DDT and [¹⁴C]cis-permethrin, suggesting the receptor binding is Ca²⁺ sensitive and may have a role in ion conductance.     

Effect of temperature on toxicity of pyrethroids and endosulfan, activity of mitochondrial Na-K-ATPase and Ca-Mg-ATPase in Chilo suppressalis (Walker) (Lepidoptera: Pyralidae)

The toxicity of deltamethrin, bifenthrin, and endosulfan to the fourth-instar larvae of rice stem borer, Chilo suppressalis (Walker), was measured at 17, 27, and 37 °C. The three insecticides all displayed a positive temperature coefficient between 17 and 37 °C. The temperature coefficients of deltamethrin, bifenthrin, and endosulfan were 5.59, 1.68, and 2.85, respectively. However, temperature coefficients of deltamethrin and bifenthrin between 17 and 27 °C and between 27 and 37 °C varied. The inhibition of the above three insecticides to mitochondrial Na⁺-K⁺-ATPase and Ca²⁺-Mg²⁺-ATPase from the fourth-instar larvae of rice stem borer was determined at 17, 27, and 37 °C. The inhibition of deltamethrin to the specific activities of Na⁺-K⁺-ATPase and Ca²⁺-Mg²⁺-ATPase showed a negative temperature coefficient, but endosulfan exhibited a positive temperature coefficient. Inhibition of bifenthrin exhibited the contrary temperature coefficients between Na⁺-K⁺-ATPase and Ca²⁺-Mg²⁺-ATPase and a negative temperature coefficient for the former and a positive temperature coefficient for the later.     

Action of cismethrin and deltamethrin on functional attributes of isolated presynaptic nerve terminals from rat brain

Isolated presynaptic nerve terminals (synaptosomes) prepared from rat brain were used to evaluate the actions of a tremor (T)-syndrome (cismethrin) and a choreoathetosis-salivation (CS)-syndrome (deltamethrin) pyrethroid on the functional attributes of synaptosomes by measuring calcium influx and endogenous neurotransmitter (l-glutamate) release with fluorescent assays. Both cismethrin and deltamethrin stimulated calcium influx, however, only deltamethrin enhanced Ca²⁺-dependent neurotransmitter release and its action was stereospecific, concentration-dependent, stimulated by depolarization, unaltered by tetrodotoxin, and blocked by ω-conotoxin GVIA. Our results delineate a separate action of deltamethrin on presynaptic nerve terminals from that elicited by cismethrin and implicate Ca_v2.2 calcium channels as target sites for deltamethrin that is consistent with the observed in vivo release of neurotransmitter at the onset of convulsive symptom caused by CS-syndrome pyrethroids. This information will allow a more complete understanding of the molecular and cellular nature of pyrethroid-induced neurotoxicity and expands our knowledge of the structure–activity relationships of pyrethroids in regards to their action on voltage-sensitive calcium channels.     

盐基离子对土壤持水及收缩特性的影响

不同盐离子对土壤持水能力具有不同程度影响,且在土壤水分特征曲线测定过程中,土体随失水发生收缩和开裂。在已获取研究成果基础上进行扩展,进一步探索8种低浓度盐离子(K~+、Na~+、Ca~(2+)、Mg~(2+)、Cl~-、HCO_3~-、CO_3~(2-)、SO_4~(2-))对土壤持水能力和收缩特征的影响。选取陕西粉黏壤土并分别采用含有此8种离子的盐溶液(浓度均约为1 g·L~(-1))对土样进行饱和处理,以无盐离子处理作为对照(CK);采用离心机法获取土壤水分特征曲线,使用游标卡尺测定离心过程中的土体轴向沉降高度,编写MATLAB程序对裂缝图像提取裂隙度量指标,据此对各处理土壤持水能力和收缩特征进行对比分析及评价。结果发现,在此浓度条件下:(1)K~+、Na~+及4种阴性盐离子在一定程度上均可提高土壤持水能力,且阴阳盐离子中CO_3~(2-)和K~+效果最显著,分别较CK提高35.81%和3.68%;(2)Mg~(2+)、SO_4~(2-)和CO_3~(2-)有利于减小土体轴向收缩度,且阴阳盐离子的作用效果分别表现为HCO_3~-Cl~-SO_4~(2-)CO_3~(2-)和Na~+K~+Ca~(2+)Mg~(2+);(3)Na~+、Mg~(2+)及4种阴性盐离子在一定程度上均有利于减轻土壤开裂程度,可同时减小土壤裂隙总长度、总面积以及长度密度和面积密度,且阴阳盐离子中CO_3~(2-)和Na~+效果最显著。研究可为不同类型盐碱土壤持水能力评价及其干缩开裂机理认知提供理论指导。     

Electrophysiological identification of site-insensitive mechanisms in knockdown-resistant strains (kdr,super-kdr) of the housefly larva (Musca domestica)

The effects of pyrethroids were studied upon isolated segmental nerves and neuromuscular junctions in both susceptible (Cooper) and knockdown-resistant (kdr; super-kdr) strains of housefly larvae (Musca domestica L.). Isolated segmental nerves contained neither cell bodies nor synaptic contacts; thus, any effects of pyrethroids were attributed solely to their actions upon voltage-dependent Na⁺ channels. Threshold concentrations of the type II pyrethroid, deltamethrin, required to elevate the spontaneous firing rate of these nerves were determined. Both resistant strains were about ten times less sensitive to deltamethrin than the susceptible strain, but insensitivity of super-kdr nerves was no greater than in the less resistant kdr strain. At neuromuscular junctions, the minimum concentrations of pyrethroids needed to trigger massive increases in the frequency of miniature excitatory postsynaptic potentials (mEPSPs) were determined for deltamethrin and the type I pyrethroid, fenfluthrin. With fenfluthrin there was no detectable difference between the junctions of kdr and super-kdr strains, which were both about ten-fold less sensitive than Cooper junctions. With deltamethrin, kdr junctions were about 30 times less sensitive than those of Cooper; super-kdr junctions were dramatically insensitive to deltamethrin, being some 10000- and 300-fold less sensitive than those of Cooper and kdr respectively. Thus, in the synaptic assay, super-kdr conferred an extension in resistance over kdr only against the type II pyrethroid, it being ineffective against fenfluthrin. We suggest that kdr resistance comprises at least two site-insensitive areas within the nervous system. One involves insensitivity of the Na⁺ channel and has similar efficacy in both kdr and super-kdr strains against type I and II pyrethroids; the other is associated with the presynaptic terminal and is particularly effective in super-kdr resistance against type II pyrethroids. The latter could be associated with Ca²⁺-activated phosphorylation of proteins involved with neurotransmitter release. Such phosphorylation reactions are known to be perturbed by pyrethroids, especially by type II compounds.     

Depolarization of motor nerve terminals by pyrethroids in susceptible and kdr-resistant house flies

When applied at concentrations of one nM or higher to a house fly larval neuromuscular preparation, deltamethrin (DM) and fenvalerate (FV) greatly increased miniature excitatory postsynaptic potential (mepsp) rate and blocked neuromuscular transmission. The DM-induced mepsp discharge was abolished by tetrodotoxin (TTX), removal of Ca²⁺ from the saline, or by application of hyperpolarizing stimuli to the nerve, indicating that it was due to depolarization of the presynaptic terminals. Also, in the presence of TTX, K⁺ depolarization increased mepsp rate at the same external K⁺ concentration before and after DM treatment, confirming that DM released transmitter by depolarizing the nerve terminals rather than by altering the voltage dependence of transmitter release. The potassium channel blocker tetraethylammonium (TEA) increased mepsp rate somewhat, while aconitine (20 μM), which keeps sodium channels open, increased mepsp rate consistently. Pretreatment of nerves with a subthreshold dose of TEA greatly increased the mepsp rate-increasing activity of DM and aconitine, while a subthreshold level of aconitine did not synergize DM. These observations suggest that DM, like aconitine, depolarized nerves by modifying the sodium channels. Knockdown resistant (kdr) larvae were resistant to the depolarizing action of DM and aconitine but not to that of TEA, indicating that the kdr gene produced a modified sodium channel which was less sensitive to the action of pyrethroids and aconitine. During sustained transmitter release by DM, evoked release gradually declined, resulting in a condition called early block in which spontaneous release was high and release could be evoked by electrotonic depolarization of the nerve terminals, but not by a nerve action potential. Early block was probably due to conduction block in the nerve terminals. Early block eventually gave way to late block, characterized by the decline of spontaneous release to subnormal levels and complete failure of evoked release. After late block, the calcium ionophore X-537A could not release transmitter, suggesting that late block was due to depletion of available transmitter. DM did not have a direct effect upon extrasynaptic muscle membrane. However, after late block, muscles were left insensitive to the putative transmitters glutamate and aspartate when these were bath or iontophoretically applied. A low rate of mepsps persisted after late block, indicating that the muscles were still sensitive to the natural transmitters.     

塔里木河流域水化学组成分布特征

于2010年6月对塔里木河干流及主要支流地表水进行水化学采样,共设25个点采集50个样品。分析表明：塔里木河干流水体中阳离子Na⁺+K⁺＞Ca²⁺＞Mg²⁺,与南北侧支流Na⁺+K⁺＞Mg²⁺＞Ca²⁺存在显著差异,但均以Na⁺+K⁺为主,阳离子浓度分别占干流、南北侧支流的68.6%、62.6%和62.5%。与1965年对应采样点同月份水化学成分相比,塔里木河流域主要可溶性离子浓度增幅较大,整体平均增加8.0倍,尤其是Cl^-达21.7倍,这可能是近年来塔里木河流域气温上升降水增加等自然因素,间接促进降水过程中水化学侵蚀地表可溶性物质所致。同时,流域内工农业快速发展,生活污水、工农业废水大量排放到塔里木河,这可能是影响塔里木河水质变化的重要因素之一。