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1.
Embryos of Danio rerio are highly susceptible to extracts of the plants Tephrosia vogelii and Asystasia vogeliana . The concentration of the dried extracts at which 50% of the embryos were affected (EC50) after 24 h exposure were 320 and 572 μg l−1, respectively; corresponding 50% mortality (LC50) values after 48 h exposure were 493 and 869 μg l−1. Results indicate that the use of these ichthyotoxic plants might have a severe impact on the survival of fish larvae in the field.  相似文献   

2.
Abstract: Some data on the concentration range of response and the concentration for half-response (EC50) of γ-aminobutyric acid (GABA) for the GABAA receptor are reviewed and compared. An analysis of the 36CI flux assay demonstrates that both the EC50 and the slope of a Hill plot depend on the ion influx or efflux assay time. The effects of depletion of the 36CI concentration gradient during the assay and of receptor desensitization on the result for a range of assay times are considered. The EC50 can be decreased by orders of magnitude by increasing the assay time. The EC50 measured in a finite time is less than the half-response concentration for the response(s) of the receptor. The extent of this difference depends on the receptor concentration per internal volume. The maximal decrease of EC50 depends on the rate of receptor desensitization. The computer simulations showed that a GABAA receptor with a half-response concentration of 100 μ M GABA can give 36CI flux measurements with an EC50 value 100-fold lower.  相似文献   

3.
Swim-through chemical repellency tests, using sodium lauryl sulphate (SLS), cupric acetate, and rotenone, were conducted in a specially-designed roundabout tank on horn sharks, Heterodontus francisci , swell sharks, Cephaloscylliun ventriosum , and leopard sharks, Triakis semifasciata . Effective concentration thresholds (EC50s) were calculated for two levels of response: (1) minimum noticeable and (2) strong. The SLS EC50s were: horn shark 43.6 and 174.5 ppm; swell shark 95.1 and 160.0 ppm; and leopard shark inconclusive and 113.1 ppm. No response was discernible from cupric acetate. Rotenone evoked a weak response with an EC50 of 5.7 ppm, but no strong response.
The ratio of the minimum noticeable EC50: 24-hour lethal concentration (LC50) indicated the relative repellency (compared to toxicity) of the chemicals. The ratio for SLS was 19:1 and for rotenone 57:1. SLS did not provoke a repellency response at a low enough concentration to function effectively as a classical, surrounding-cloud type, repellent. The range of potency of SLS, however, does allow it to be used as a directional repellent.  相似文献   

4.
Abstract: The effects of the nicotinic agonist (+)-anatoxin-a have been examined in four different preparations, representing at least two classes of neuronal nicotinic receptors. (+)-Anatoxin-a was most potent (EC50= 48 n M ) in stimulating 86Rb+ influx into M10 cells, which express the nicotinic receptor subtype comprising α4 and β2 subunits. A presynaptic nicotinic receptor mediating acetylcholine release from hippocampal synaptosomes was similarly sensitive to (+)-anatoxin-a (EC50= 140 n M ). α-Bungarotoxin-sensitive neuronal nicotinic receptors, studied using patch-clamp recording techniques, required slightly higher concentrations of this alkaloid for activation: Nicotinic currents in hippocampal neurons were activated by (+)-anatoxin-a with an EC50 of 3.9 γ M , whereas α7 homooligomers reconstituted in Xenopus oocytes yielded an EC50 value of 0.58 γ M for (+)-anatoxin-a. In these diverse preparations, (+)-anatoxin-a was between three and 50 times more potent than (–)-nicotine and ˜20 times more potent than acetylcholine, making it the most efficacious nicotinic agonist thus far described.  相似文献   

5.
1. Arctopsyche ladogensis , Hydropsyche angustipennis and Hydropsyche siltalai larvae were exposed to nominal aluminium concentrations of 0, 625, 1250, 2500 and 5000 μg Al l–1 at pH 5.0 for 96 h. Larvae reared at pH 6.4 and without any aluminium treatment were used as controls. Morphological abnormalities in the anal papillae of the larvae were used as the response variable in estimating the median effective concentrations (EC50) of aluminium.
2. No morphological abnormalities were observed in the control larvae. Only a few individuals of A. ladogensis had darkened anal papillae at pH 5.0 without additional aluminium treatment, whereas increasing aluminium concentrations significantly increased the number of individuals in all species displaying darkening and reduction of the papillae.
3. A. ladogensis appeared to be the most sensitive species to increasing aluminium concentrations, as reflected by the significantly lower mean EC50 value for this species compared with those of H. siltalai and H. angustipennis . H. angustipennis larvae were the most tolerant to aluminium.
4. The results indicate that interspecific differences in sensitivity to aluminium may be a key factor influencing the guild structure of filter feeding caddis flies in acidified streams. The results also imply that toxic effects of aluminium on filter feeding caddis larvae occur due to the impairment of normal osmoregulation processes via damage to the ion-regulatory organs.  相似文献   

6.
1. Arctopsyche ladogensis , Hydropsyche angustipennis and Hydropsyche siltalai larvae were exposed to nominal aluminium concentrations of 0, 625, 1250, 2500 and 5000 μg Al l–1 at pH 5.0 for 96 h. Larvae reared at pH 6.4 and without any aluminium treatment were used as controls. Morphological abnormalities in the anal papillae of the larvae were used as the response variable in estimating the median effective concentrations (EC50) of aluminium.
2. No morphological abnormalities were observed in the control larvae. Only a few individuals of A. ladogensis had darkened anal papillae at pH 5.0 without additional aluminium treatment, whereas increasing aluminium concentrations significantly increased the number of individuals in all species displaying darkening and reduction of the papillae.
3. A. ladogensis appeared to be the most sensitive species to increasing aluminium concentrations, as reflected by the significantly lower mean EC50 value for this species compared with those of H. siltalai and H. angustipennis . H. angustipennis larvae were the most tolerant to aluminium.
4. The results indicate that interspecific differences in sensitivity to aluminium may be a key factor influencing the guild structure of filter feeding caddis flies in acidified streams. The results also imply that toxic effects of aluminium on filter feeding caddis larvae occur due to the impairment of normal osmoregulation processes via damage to the ion-regulatory organs.  相似文献   

7.
Abstract: The age-specific survival and fecundity of female adults of the aphidophagous parasitoid, Aphelinus gossypii Timberlake (Hym., Aphelinidae), were determined at a host density of 50 Aphis gossypii Glover (Hom., Aphididae) per leaf of Ageratum houstonianum Mill each day at 25°C. The age-specific mummy production, emergence rate and sex ratio of progeny were calculated. The implication of these results in terms of potential population growth of A. gossypii and related species is discussed. The age-specific survival curve ( l x ) of females exhibited a Type I pattern, which resulted in little difference between Σ m x and Σ l x   m x . The l x curve of males exhibited a Type II pattern, and their survival time was much shorter than that of females. Each mated female produced on average 598.9 ± 64.0 aphid mummies, and preyed on 87.9±6.2 aphids. Most of the biological performance parameters were not different significantly between mated and virgin females. The highly female-biased sex ratio of offspring produced by mated females soon after their emergence resulted in a high fecundity rate ( m x ) during the early reproductive period. Therefore, although the sex ratio of progeny was male-biased during the entire reproductive period, the intrinsic rate of increase estimated using age-specific sex ratios was larger than that estimated using a constant sex ratio of 0.5. These results indicate that the high survival and the adaptation of producing mostly female offspring during the early reproductive period contribute much to the population increase potential of this parasitoid.  相似文献   

8.
Potential desensitization of brain nicotinic receptors was studied using a [3H]dopamine release assay. Nicotine-stimulated [3H]dopamine release from mouse striatal synaptosomes was concentration-dependent with an EC50 of 0.33 ± 0.13 μ M and a Hill coefficient of 1.44 ± 0.18. Desensitization by activating concentrations of nicotine had a similar EC50 and a half-time of 35 s. Concentrations of nicotine that evoked little release also induced a concentration-dependent desensitization (EC50=6.9 plusmn; 3.6 n M , t1/2= 1.6-2.0 min, n H=1.02 ± 0.01). Both types of desensitization produced a maximum 75% decrease in [3H]dopamine release. Recovery from desensitization after exposure to low or activating concentrations of nicotine was time-dependent with half-times of 6.1 min and 12.4 min, respectively. Constants determined for binding of [3H]nicotine to striatal membrane at 22°C included a K Dof 3.7 ± 0.5 n M , Bmax of 67.5 ± 2.2 fmol/mg, and Hill coefficient of 1.07 ± 0.06. Association of nicotine with membrane binding sites was biphasic with half-times of 9 s and 1.8 min. The fast rate process contributed 37% of the total reaction. Dissociation was a uniphasic process with a half-time of 1.6 min. Comparison of constants determined by the release and binding assays indicated that the [3H]-nicotine binding site could be the presynaptic receptor involved in [3H]dopamine release in mouse striatal synaptosomes.  相似文献   

9.
Abstract: A charybdotoxin-sensitive, Ca2+-activated K+ channel was identified in cultured rat brain capillary endothelial cells by using conventional single-channel recording techniques and 86Rb+-influx and efflux experiments. Channel activity was dependent on the presence of Ca2+ on the cytosolic face of the membrane with a threshold concentration of 100 n M . It was inhibited by charybdotoxin (IC50 30 n M ) and quinine (IC50 0.1 m M ) but not by apamin. K(Ca) channels showed unusual inward rectifying properties under asymmetrical ionic conditions. They were activated by endothelin-1 (EC50 0.7 n M ) and endothelin-3 (EC50 7–10 n M ). The actions of endothelins were prevented by BQ-123 ( K i = 8 n M ) in a competitive fashion, hence suggesting the involvement of an ETA-receptor subtype. The channel activity was unaffected by cyclic AMP- or cyclic GMP-elevating agents. The possible role of the intermediate conductance, Ca2+-activated K+ channels for mediating K+ movements across the blood-brain barrier is discussed.  相似文献   

10.
In this study, we investigate the effects of chronic administration of (−)nicotine on the function of the NMDA-mediated modulation of [3H]dopamine (DA) release in rat prefrontal cortex (PFC) and nucleus accumbens (NAc). In the PFC synaptosomes NMDA in a concentration-dependent manner evoked [3H]DA release in rats chronically treated with vehicle (14 days) with an EC50 of 13.1 ± 2.0 μM. The NMDA-evoked overflow of the [3H]DA in PFC nerve endings of rats treated with (−)nicotine was significantly lower (−43%) than in vehicle treated rats. The EC50 was 9.0 ± 1.4 μM. Exposure of NAc synaptosomes of rats treated with vehicle to NMDA produced an increase in [3H]DA overflow with an EC50 of 14.5 ± 5.5 μM. This effect was significantly enhanced in chronically treated animals. The EC50 was 10.5 ± 0.5 μM. The K+-evoked release of [3H]DA was not modified by the (−)nicotine administration. Both the changes of the NMDA-evoked [3H]DA overflow in the NAc and PFC disappeared after 14 days withdrawal. The results show that chronic (−)nicotine differentially affects the NMDA-mediated [3H]DA release in the PFC and NAc of the rat.  相似文献   

11.
The biological control potential of Pochonia chlamydosporia against root-knot ( Meloidogyne spp.) and cyst-forming ( Heterodera and Globodera spp.) nematodes is widely appreciated. In spite of this, little has been undertaken to determine the compatibility of this fungus with modern fungicides. A series of experiments were undertaken to investigate the effect of azoxystrobin on P. chlamydosporia . Initial Petri dish experiments found a significant reduction in the growth of P. chlamydosporia . EC50 values were calculated at 7 and 14 mg L−1, respectively, for hyphal growth and chlamydospore germination. A microcosm experiment based on counts of the colony-forming units of the re-isolated fungus showed a reduction in EC50 values for azoxystrobin in soil after 12, 20 and 40 days incubation (1.25, 1.00 and 3.00 mg kg−1 soil, respectively). There was evidence the fungus recovered over time in response to azoxystrobin application. This was also demonstrated in a glasshouse experiment where EC50 values of 1.32 and 4.4 mg kg−1 soil were obtained for 35 and 49 days after planting (DAP), respectively.  相似文献   

12.
13.
Abstract: This study examined γ-aminobutyric acidA (GABAA) receptor function in cultured rat cerebellar granule cells by using microphysiometry following chronic flunitrazepam exposure, and correlated the findings with the α1 and β2/3 subunit protein expression and [3H]muscimol binding after the same treatment paradigm. Flunitrazepam treatment reduced ( p < 0.05) the maximal GABA-stimulated increase in extracellular acidification rate ( E max) (16.5 ± 1.2% and 11.3 ± 1.0%, 2-day control and treated cells, respectively; 17.4 ± 1.0% and 9.9 ± 0.7%, 7-day control and treated cells, respectively; best-fit E max± SEM, n = 7), without affecting the GABA concentration required to elicit 50% of maximal response (EC50) (1.2 ± 1.7 and 2.3 ± 1.8 µ M , 2-day control and treated cells, respectively; 1.7 ± 1.5 and 1.5 ± 1.5 µ M , 7-day control and treated cells, respectively; best-fit EC50± SEM, n = 7). Flunitrazepam exposure also abolished the flunitrazepam potentiation of the GABA response, caused a transient reduction of the GABAA receptor α1 and β2/3 subunit proteins over the initial 2 days, but did not alter [3H]muscimol binding compared with vehicle-treated cells. The results suggest that changes in GABAA receptor subunit protein expression, rather than loss of [3H]muscimol binding sites, underlie the chronic flunitrazepam-mediated desensitisation of GABAA receptor function.  相似文献   

14.
Abstract: Different neurotransmitter receptor agonists [carbachol, serotonin, noradrenaline, histamine, endothelin-1, and trans -(1 S ,3 R )-aminocyclopentyl-1,3-dicarboxylic acid ( trans -ACPD)], known as stimuli of phospholipase C in brain tissue, were tested for phospholipase D stimulation in [32P]Pi-prelabeled rat brain cortical and hippocampal slices. The accumulation of [32P]phosphatidylethanol was measured as an index of phospholipase D-catalyzed transphosphatidylation in the presence of ethanol. Among the six neurotransmitter receptor agonists tested, only noradrenaline, histamine, endothelin-1, and trans -ACPD stimulated phospholipase D in hippocampus and cortex, an effect that was strictly dependent of the presence of millimolar extracellular calcium concentrations. The effect of histamine (EC50 18 µ M ) was inhibited by the H1 receptor antagonist mepyramine with a K i constant of 0.7 n M and was resistant to H2 and H3 receptor antagonists (ranitidine and tioperamide, respectively). Endothelin-1-stimulated phospholipase D (EC50 44 n M ) was not blocked by BQ-123, a specific antagonist of the ETA receptor. Endothelin-3 and the specific ETB receptor agonist safarotoxin 6c were also able to stimulate phospholipase D with efficacies similar to that of endothelin-1, and EC50 values of 16 and 3 n M , respectively. These results show that histamine and endothelin-1 stimulate phospholipase D in rat brain through H1 and ETB receptors, respectively.  相似文献   

15.
Abstract: In cultured bovine adrenal medullary cells, stimulation of nicotinic receptors by carbachol evoked the Ca2+-dependent exocytotic cosecretion of proadrenomedullin N-terminal 20 peptide (PAMP) (EC50 = 50.1 µ M ) and catecholamines (EC50 = 63.0 µ M ), with the molar ratio of PAMP/catecholamines secreted being equal to the ratio in the cells. Addition of PAMP[1–20]NH2 inhibited carbachol-induced 22Na+ influx via nicotinic receptors (IC50 = 2.5 µ M ) in a noncompetitive manner and thereby reduced carbachol-induced 45Ca2+ influx via voltage-dependent Ca2+ channels (IC50 = 1.0 µ M ) and catecholamine secretion (IC50 = 1.6 µ M ). It did not alter high K+-induced 45Ca2+ influx via voltage-dependent Ca2+ channels or veratridine-induced 22Na+ influx via voltage-dependent Na+ channels. PAMP seems to be a novel antinicotinic peptide cosecreted with catecholamines by a Ca2+-dependent exocytosis in response to nicotinic receptor stimulation.  相似文献   

16.
The importance of xylem constraints in the distribution of conifer species   总被引:10,自引:0,他引:10  
Vulnerability of stem xylem to cavitation was measured in 10 species of conifers using high pressure air to induce xylem embolism. Mean values of air pressure required to induce a 50% loss in hydraulic conductivity (φ50) varied enormously between species, ranging from a maximum of 14.2±0.6 MPa (corresponding to a xylem water potential of −14.2 MPa) in the semi-arid species Actinostrobus acuminatus to a minimum of 2.3±0.2 MPa in the rainforest species Dacrycarpus dacrydioides . Mean φ50 was significantly correlated with the mean rainfall of the driest quarter within the distribution of each species. The value of φ50 was also compared with leaf drought tolerance data for these species in order to determine whether xylem dysfunction during drought dictated drought response at the leaf level. Previous data describing the maximum depletion of internal CO2 concentration (ci) in the leaves of these species during artificial drought was strongly correlated with φ50 suggesting a primary role of xylem in effecting leaf drought response. The possibility of a trade-off between xylem conductivity and xylem vulnerability was tested in a sub-sample of four species, but no evidence of an inverse relationship between φ50 and either stem-area specific (Ka) or leaf-area specific conductivity (K1) was found.  相似文献   

17.
The toxicity of two common organotin pollutants and their initial breakdown products (tributyltin, dibutyltin, triphenyltin and diphenyltin) were assessed using two different bioluminescent microbial biosensors: Microtox and lux -modified Pseudomonas fluorescens pUCD 607. The organotins were made up as standards, and tested both in double-deionized water and in extracted soil solution, the latter representing a realistic matrix for terrestrial contamination. Microtox was especially sensitive to the organotins, with 50% effective concentration (EC50) values (15 min) for tributyltin as low as 21·9 μg l−1 in pure water, and 0·118 μg l−1 in soil extract. The sensitivity of Microtox was increased by an order of magnitude in soil extract. The Ps. fluorescens was less sensitive, with EC50 values (30 min) of around 800 μg l−1 in pure water. The toxicity to Ps. fluorescens was decreased by around an order of magnitude in soil extract. The two biosensors showed different response patterns, with Microtox being more sensitive to the triorganotins and Ps. fluorescens being more sensitive to the diorganotins.  相似文献   

18.
Abstract: Little is known about the coupling of serotonin 5-HT1B receptors to cellular signals other than cyclic AMP. In the present studies, the activation by 5-HT1B receptors of p70 S6 kinase and the mitogen-activated protein kinase (MAP kinase) ERK-2 was investigated. Studies were performed by using both nontransfected Chinese hamster ovary (CHO) cells, which express endogenous receptors at a very low density, and a stable transfected CHO cell line expressing 5-HT1B receptors at 230 fmol/mg of membrane protein, a density similar to that expressed in cortex. In nontransfected cells, 5-HT was found to stimulate a greater than twofold increase in MAP kinase activity with an EC50 of 20 n M . Reflecting increased density of receptors, 5-HT caused a greater than eightfold activation of ERK-2 in transfected cells with an EC50 of 2 n M . 5-HT was found to also stimulate p70 S6 kinase in both nontransfected and transfected cells. The stimulation was sixfold in both types of cells, but the EC50 for 5-HT was fourfold lower in transfected cells. The coupling of 5-HT1B receptors to ERK-2 and to p70 S6 kinase was inhibited by pertussis toxin, inhibitors of phosphatidylinositol 3-kinase, and by the inhibitor of MAP kinase kinase PD098059. Activation of p70 S6 kinase, but not ERK-2, was also inhibited by rapamycin. These findings demonstrate that 5-HT1B receptors couple to ERK-2 and p70 S6 kinase through overlapping, but nonidentical, pathways.  相似文献   

19.
Abstract: In the rat parotid gland, the neuropeptide substance P (SP), as well as SP(4–11), and septide elicited inositol phosphate production (EC50 values 0.44, 2, and 20 n M , respectively). No additivity of the maximal response to the three agonists was observed. SP, SP(4–11), and septide also stimulated protein secretion; for SP, two EC50 were determined (0.5 and 160 n M ), whereas a single one could be determined for SP(4–11) and septide (EC50 values 15 and 20 n M , respectively). The selective tachykinin NK1 receptor antagonist RP67580 acted as a competitive inhibitor of both SP- and SP(4–11)-induced inositol phosphate production. Its effect on septide-induced inositol phosphate production was noncompetitive. RP67580 is apparently as potent at antagonizing septide, SP, or SP(4–11) (in all cases K B = 3 n M ). These results show that in parotid gland, only NK1 receptors are activated by SP, SP(4–11), and septide. We also showed that the protein secretion stimulated by SP was inhibited competitively by RP67580, whereas the effect of RP67580 was noncompetitive on protein secretion when SP(4–11) or septide was used. Our data indicate that in rat parotid gland, the existence of a specific "septide-sensitive" receptor can be ruled out and that only the NK1 receptor is present and mediates cellular responses. Taken together, these results show that in this tissue the NK1 receptor would present at least two different binding sites that could be coupled to different transduction pathways and that would regulate protein secretion.  相似文献   

20.
Efficacy of two tropical plant extracts for the control of mosquitoes   总被引:10,自引:0,他引:10  
The larvicidal activity of seed and leaf extracts of Calophyllum inophyllum and leaf extract of Rhinacanthus nasutus on the juveniles of Culex quinquefasciatus , Anopheles stephensi and Aedes aegypti was determined. Ethyl acetate (EA) soluble fractions of C. inophyllum and petroleum ether (PE) fraction of R. nasutus extracts showed very high larvicidal activity. Irrespective of the species of the mosquitoes tested, at concentrations ranging from 3.91 to 9.39 ppm, 9.04 to 35.49 ppm and 13.21 to 28.92 ppm of the active fractions of seed and leaf extracts of C. inophyllum and the leaf extract of R. nasutus , respectively, killed 50% of the treated larvae. The fractions also interfered with adult emergence. Exposure of the mosquitoes at any stage of their larval development to less than 0.86, 5.49 and 6.81 ppm of the active fractions of seed and leaf extracts of C. inophyllum and the leaf extract of R. nasutus , respectively, inhibited 50% of the treated larvae from emerging as adults. Experiments under laboratory and semi-field conditions showed that the activity of the extracts persisted for up to 10 days.  相似文献   

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