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1.
A single oral dose of 0.14 mg kg?1 of [14C] flocoumafen to rat, which gave a transient, non-lethal, effect, was rapidly absorbed, radioactivity appearing in the blood maximally at 4 h and falling to half maximum value by 8 h. The maximum effect on prothrombin time was at 24 h and the value returned to normal by 48 h. Elimination of radioactivity was very slow, with less than 0.5% of the dose in the urine up to 7 days after dosing, and 23-26% in the faeces (more than half of which appeared in the first 24 h). Most of the administered radioactivity (74-76%) was retained 7 days after dosing. Approximately half of the dose was in the liver; it was eliminated with a halflife of 220 days. At 48 h after dosing, most of the hepatic radioactivity comprised unchanged flocoumafen. Treatments of flocoumafen-dosed rats with warfarin or with cytochrome P450-inducing doses of phenobarbitone were without effect on the hepatic residue of flocoumafen.  相似文献   

2.
A blood-clotting response test for warfarin resistance in Norway rats ( Rattus norvegicus ) was developed by our laboratory in the late 1970s, based on knowledge of biochemical mechanisms available at that time. That test used warfarin, its the free base which is not watersoluble, and vitamin K1 2,3-epoxide as an antidote for warfarin-resistant rats only. We have modified the above test to use a water-soluble salt of vitamin K3 (1 mg kgg−1 body weight), which is an antidote in a wider range of warfarin-resistant rat strains than vitamin K1 2,3- epoxide, and a water-soluble salt of warfarin (5.4 mg kg−1 body weight). Sodium warfarin and vitamin K3 are administered by oral gavage, and the blood-clotting response measured 24 h later. In a series of validation tests there were no significant differences between results obtained by either method. The new method, however, uses materials which are commercially available, and eliminates the possibility of misclassifying warfarin-resistant rats as susceptible because vitamin K1 2,3-epoxide was not an antidote in those strains. We also present evidence that measuring blood-clotting response to feeding on a vitamin K-free diet for 4 days is not a reliable method for determining the genotype of warfarin-resistant rats.  相似文献   

3.
洞庭湖区东方田鼠对敌鼠钠盐的敏感性分析   总被引：1，自引：0，他引：1  
为了有效使用抗凝血灭鼠剂防治鼠害,采用强制喂食法将0.025％敌鼠钠盐毒饵分别连续喂食不同性别的成年东方田鼠1、2、4、6和8d,记录东方田鼠取食和死亡情况,并分析洞庭湖区东方田鼠对敌鼠钠盐的敏感性.结果显示:东方田鼠的毒饵取食量有下降的趋势,但不显著;不同性别东方田鼠对敌鼠钠盐的敏感性无显著差异,合并雌、雄东方田鼠数据,其LFP50和LFP99的估计值分别为0.60 d和5.70 d;东方田鼠取食毒饵后,死亡高峰期出现在第4～7天.研究表明洞庭湖区东方田鼠对敌鼠钠盐无抗性,0.025％敌鼠钠盐能够有效防治该地区东方田鼠.  相似文献   

4.
California voles cause damage to pastures and rangelands, orchards and nurseries, and a wide variety of field crops, including artichokes. The anticoagulant rodenticides (chlorophacinone and diphacinone) typically used for voles are becoming less effective in controlling their populations. Consequently, there is a need to identify new rodenticides that will have a high efficacy on California voles so that agricultural production losses to rodents can be substantially reduced. We tested a new formulation containing two active ingredients (cholecalciferol and diphacinone) as a control method for California voles. Both a pelleted bait and an oil-coated artichoke bract bait were very palatable and efficacious against wild-caught, captive California voles. Efficacy levels of 70%–80% were achieved in the two-choice feeding trials. Additionally, the days-to-death (5–6 days) were less than the time-to-death with anticoagulant only baits. We recommend that a field efficacy study be conducted with cholecalciferol plus diphacinone bait formulations to determine their field performance in the reduction of agricultural damage by California voles.  相似文献   

5.
The metabolism of benodanil (2-iodobenzanilide) was studied in rats following an oral dose of 150 mg benodanil kg?1 body weight. The major 24-h urinary metabolite was found to be the 4′-hydroxy derivative, both free (≈ 5%) and as the glucuronide (≈ 4%) and sulphate (≈ 4%) conjugates. Over a 6-day period, about 16% of the administered dose was excreted in the urine and about 80% in the faeces. After dosing with [14C]- benodanil, blood radioactivity levels were highest 30 min after dosing, with small broader peaks at 4 and 7 h, while biliary activity levels rose slowly to a maximum about 10–12 h after the dose, some 16% being excreted in 24 h as the glucuronide conjugate of the 4′-hydroxy derivative.  相似文献   

6.
Tissue distribution and excretion of the rodenticide, [14C] diphacinone (2-diphenylacetyl-1,3-indandione), following intragastric administration were investigated in male and female mice. The first body burden study tested 13 tissues plus excreta and utilized tissue digestion prior to counting. Plasma and whole blood were additionally tested in the second study; tissues and excreta were prepared for counting in a commercial sample oxidizer. Of the administered dose 76 and 68% were excreted in feces of male and female mice, respectively, by 48 hr during the first study. Accountability of the administered dose never exceeded 74%. The two studies revealed that liver had the highest specific activity followed by fallopian tubes, plasma, whole blood, and lungs. Adipose tissue contained the lowest concentration. In the second study, the specific activity increased in male liver up to 7.5 hr. Radioactivity in female livers peaked around hr 3. These were the only significant differences between sexes.  相似文献   

7.
目前在美国环保署登记应用的杀鼠剂商品共有302个,有效成分13种。其中磷化锌、氯鼠酮、敌鼠酮、α-氯代醇和马钱子碱等全部或部分产品被列入限制使用农药产品名录,和其他限制使用农药一样受到限制使用政策的约束。同时,美国杀鼠剂产品的销售、流通和使用主要受到EPA《杀鼠剂风险消减决定》的限制,特别是第二代抗凝血类药剂只允许在特定专业领域流通和使用。  相似文献   

8.
The penetration and metabolism of [14C]deltamethrin was studied in susceptible and resistant Chinese and Pakistani strains of Helicoverpa armigera (Hübner), which were resistant to deltamethrin by 330- and 670-fold, respectively. The penetration of deltamethrin into resistant individuals was significantly slower than into susceptible individuals over a 24-h period. The time taken for 50% penetration of the applied deltamethrin was 1 h for the susceptible strain and 6 h for both of the resistant strains. The internal radioactivity was reduced by the larvae of resistant strains much faster than by the susceptible larvae. After 48 h, 40% of the penetrated deltamethrin was still inside the larvae of the susceptible strain, in comparison with 1.5-5% in the Pakistani strain and 8-14% in the Chinese strain. Both of the resistant strains produced methanol-soluble and water-soluble metabolites, but the susceptible strain produced methanol-soluble metabolites only. By 12, 24 and 48 h after dosing, the amount of methanol-soluble metabolites excreted by the resistant strains was almost double that of the susceptible strain. Both of the resistant strains also excreted 5-7% of the penetrated dose as a water-soluble metabolite after 48 h. In comparison with the Chinese strain, the Pakistani strain exhibited slower penetration, lower internal content and faster excretion of deltamethrin, which correlated with the higher resistance of the Pakistani strain. These findings show that the resistant Pakistani and Chinese strains of H. armigera possess mechanisms of reduced cuticular penetration and enhanced metabolism of deltamethrin and perhaps other pyrethroids.  相似文献   

9.
Two squirrels aged 16 weeks and three muskrats aged 24 weeks were subcutaneously infected with a dose of 400 SMicLD50 of the extraneurally passaged "236" strain of Tahyna virus. Viremia was detected in one squirrel (48 and 96 hours post infection) and in two muskrats (24 and 48 hours p.i.). Seroconversion was demonstrated by plaque-reduction neutralization test (PRNT) 21 days p.i. in all animals.  相似文献   

10.
There are two recognized forms of the disease net blotch of barley: the net form caused by Pyrenophora teres f. teres (PTT) and the spot form caused by P. teres f. maculata (PTM). In this study, amplified fragment length polymorphism analysis was used to investigate the genetic diversity and population structure of 60 PTT and 64 PTM isolates collected across Australia (66 isolates) and in the south‐western Cape of South Africa (58 isolates). For comparison, P. tritici‐repentis, Exserohilum rostratum and Bipolaris sorokiniana samples were also included in the analyses. Both distance‐ and model‐based cluster analyses separated the PTT and PTM isolates into two strongly divergent genetic groups. Significant variation was observed both among the South African and Australian populations of PTT and PTM and among sampling locations for the PTT samples. Results suggest that sexual reproduction between the two forms is unlikely and that reproduction within the PTT and PTM groups occurs mainly asexually.  相似文献   

11.
A 6-year study led to the development of a tomato seed treatment that controlledPseudomonas syringae pv.tomato (PT),Pseudomonas corrugata (PC),Xanthomonas campestris pv.vesicatoria (XV), andClavibacter michiganense subsp.michiganense (CM). Tomato seeds were immersed, at a ratio of 1:4 (w/v) seeds: chemical, in a solution containing cupric acetate, acetic acid, pentachloronitrobenzene, 5-ethoxy-3(trichloromethyl)-l,2,4-thiadiazole, and Triton x-100, for 1 h at 45±0.1 °C. The treatment was carried out in a thermostat-controlled bath circulator. The pathogens PT, XV and CM were almost eradicated after immersion of seeds for 30 min at 25 °C, whereas PC was controlled only after 1 h of treatment at 45 °C. The effectiveness of the treatment was related to the formation of a Cu2+ organic complex in the solution. The treatment did not affect seed germination or seedling vigor. Most of the tomato seeds produced or imported by Israel are now successfully treated by this method.  相似文献   

12.
[14C]Flamprop-methyl administered orally to rats (3-4 mg kg?1 body weight) was excreted mostly via the faeces (78.7 and 61.6% in males and females, respectively). Elimination was rapid and 90% of the dose of 14C was excreted in faeces and urine 0-48 h after dosing. The distribution of 14C between faeces and urine was different in males and females. No expired [14C]carbon dioxide was detected and less than 2% of the dose remained in the animals 4 days after dosing. The predominant metabolic pathway was hydrolysis of the ester bond to afford the carboxylic acid which was excreted unchanged and as its glucuronide conjugate. Aromatic hydroxylation occurred at the para- and meta-positions of the N-benzoyl ring. N-(3)-Chloro- 4-fluorophenyl-N-(3,4-dihydroxybenzoyl)-DL -alaninate was also formed. This hydroxylated form of flamprop-methyl was partially O-methylated at the 3-hydroxy group. Flamprop-methyl was also metabolised and eliminated rapidly by dogs, mice and rabbits. The last of these three species afforded very little aromatic hydroxylation and also differed from the others in that the metabolites were eliminated mostly in the urine. Aromatic hydroxylation lay in the order: male rat = female rat > dog= mouse>rabbit (female).  相似文献   

13.
A single dose (4 mg kg?1) of 14 C-labelled (R)-flamprop-methyl to rat was rapidly metabolised and 90% of the dose was eliminated in urine and faeces within 48 h. Four days after dosing, tissue residues were 0–1 μg equivalents g?1 tissue or much less, with the exception of kidney (0–22 μg g?1). There was a statistically significant sex difference in the routes of elimination; this may be attributed to differences in the biliary elimination of the major metabolite, flamprop acid, or its glucuronide conjugate. The fate of racemic flamprop-methyl was very similar to that of the (R)-isomer. The major metabolic routes were hydrolysis of the esters to the corresponding acids, hydroxylation of the benzoyl aromatic rings and conjugation. The flamprop acid derived from the (R)-flamprop-methyl was found to be partially converted to the (S)-form (R:S ratio, 87:13). This reaction is discussed in the context of other such biological racemisations recently reported.  相似文献   

14.
The uptake, accumulation, metabolism and excretion of gamma-HCH (the gamma isomer of 1,2,3,4,5,6-hexachlorocyclohexane) by a highly gamma-HCH-resistant strain of Sitophilus granarius was studied. It was found that the resistant strain was able to excrete a large proportion of a topically-applied dose of gamma-HCH in its frass pellets; under comparable conditions a susceptible strain accumulated a high body load of gamma-HCH. Neither strain metabolised gamma-HCH to any significant extent over a 48-h period after dosing.  相似文献   

15.
We investigated the genotypes of Cryptosporidium infecting red squirrels (Sciurus vulgaris L.) in two areas of the Western Alps in Italy. Examination of 141 faecal samples from 70 red squirrels revealed oocysts of Cryptosporidium in 17 animals (24.3%). Based on 18S rRNA gene sequencing, two genotypes of Cryptosporidium species were found: 15 squirrels were positive for the Cryptosporidium ferret genotype and 2 for the Cryptosporidium chipmunk genotype I. The occurrence and intensity of Cryptosporidium infection did not differ between the study areas or sex. More than 85% of the positive animals were adults; however no difference was found between Cryptosporidium infection in the juvenile and adult age groups. Oocysts of the Cryptosporidium ferret genotype measured 5.5 +/- 0.3 x 5.2 +/- 0.2 microm (shape index 1.06) and the Cryptosporidium chipmunk genotype I 5.8 +/- 0.3 x 5.4 +/- 0.3 microm (shape index 1.07). Neonatal and adult CD1 and BABL/c mice inoculated with 1 x 10(3) fresh oocysts of both genotypes did not produce detectable infection.  相似文献   

16.
The effect of single, binary, and tertiary combination of few plant derived molluscicides alone or in combination with synergist on different enzymes (acetylcholinesterase—AChE, lactic dehydrogenase—LDH, and acid/alkaline phosphatase—ACP/ALP in the nervous tissue of the freshwater snail Lymnaea acuminata were studied. Sublethal in vivo 24 h exposure to 40 and 80% of LC50 of Azadirachta indica oil (AI), oleoresin of Zingiber officinale (OL), Cedrus deodara oil (CD), Allium sativum (AS), and Polianthes tuberosa (PT) bulb powder singly, their binary combination of AI + OL, AS + CD, AS + PT, CD + OL, CD + PT, OL + PT, and tertiary combination of these binary combinations with the synergist piperonyl butoxide (PB) or MGK-264 significantly altered the activity of these enzymes. Tertiary combination with PB or MGK was very effective. Combination of CD + PT + MGK was more effective against AChE whereas, the combination of CD + OL + PB, CD + AS + PB, and CD + PT + PB were more effective against LDH, ACP, and ALP, respectively.  相似文献   

17.
The disposition of the pyrethroid insecticide cypermethrin, (RS)-a-cyano-3-phenoxybenzyl (1RS)-cis, trans-3-(2,2-dichlorovinly)-2, 2-dimethylcyclopropane-carboxylate, has been studied in male and female rats following a single toxic oral dose (200mg kg−1) of two radiolabelled forms ([14C-benzyl] and [14C-cyclopropyl]) of the insecticide. The bioaccumulation and elimination of 14C-benzyl-labelled cypermethrin, following repeated administration at a sub-toxic dose (2mg kg−1), has also been studied in male and female rats. Although, at the toxic dose, radioactivity from the two radiolabelled forms was rapidly eliminated in urine and faeces, the increased excretion in the faeces, over that for low doses, was evidence that absorption was incomplete. The major pathways of metabolism involved cleavage of the ester bond, with subsequent hydroxylation and glucuronidation of the cyclopropyl acid moieties, together with hydroxylation and sulphation of the 3-phenoxybenzyl moiety. The absence of sex- or dose-dependent changes was reflected by the constant proportions of these metabolites found in the urine. Constant levels of radioactivity in tissues were achieved rapidly, generally within the first week of repeated administration. Elimination was rapid on the cessation of dosing, although less rapid from the fat and skin. The material in the fat was mainly the cis-isomers of cypermethrin, which were eliminated with a mean half-life of 18.2 days, compared with 3.4 days for the trans-isomers.  相似文献   

18.
Pharmacokinetic properties and tissue residues of the insecticide sulfluramid (I) and its major metabolite desethylsulfluramid (II) were determined in healthy sheep after bolus intravenous (IV) administration (5 and 15 mg kg−1; n = 10) and bolus intraruminal (IR) administration (100 and 400 mg kg−1; n = 12) of I . Depression, lethargy, and dyspnea were noted for 4 h after the higher IV dose, but not after the other IV or IR doses. The time courses of the mean blood concentrations of I and II were best described by a two-compartment open model with rapid distribution and slow elimination phases. The blood-to-plasma concentration ratios for I and II were 1.43 (± 0.50) and 26.7 (± 9.41), respectively, suggesting binding of II to red blood cells. The T1/2β values for I and II for the higher IV dose of I were 15.3 (± 4.68) h and 63.4 (± 4.75) h and for the higher IR dose of I , 31.5 (± 5.41) h and 74.9 (± 7.49) h, respectively. Bioavailability was 28.6 (± 2.96)% for the lower IR dose and 19.5 (± 0.99)% for the higher IR dose. Cmax values for II were higher in female than male sheep after IR administration of I . Only II was found in tissue samples, with the highest concentration being in liver (9.4 (± 5.2) µg g−1). © 1999 Society of Chemical Industry  相似文献   

19.
球孢白僵菌是一种对西花蓟马具高致病力的重要生防真菌。球孢白僵菌感染改变了西花蓟马的偏好温度。探讨这一现象对于提高球孢白僵菌对西花蓟马的防治效果具有重要意义。本研究分析了西花蓟马偏好温度随球孢白僵菌剂量和感染时间的变化趋势。结果表明,在各观察时间点（24～120 h,48 h除外）,感染高剂量球孢白僵菌的西花蓟马偏好温度显著低于被低剂量真菌侵染的个体。与健康西花蓟马的偏好温度（24℃±0.5℃）相比,无论是高剂量还是低剂量真菌,染菌蓟马偏好温度均随时间推移呈先下降后上升的趋势。染菌0～48 h时,蓟马的偏好温度逐渐下降。染菌后48～120 h,偏好温度回升。感染高剂量球孢白僵菌的蓟马体内真菌基因拷贝数大于被低剂量真菌感染的个体,随染菌时间的推移,差异进一步加大。本研究将为建立西花蓟马的高效防控体系提供理论支持。  相似文献   

20.
麻疯树萜醇I对家蚕的毒性及作用机理研究   总被引：14，自引：0，他引：14  
研究了从麻疯树种子中分离的麻疯树萜醇I对3龄家蚕的毒性及其对家蚕中肠蛋白酶和组织结构的影响。结果显示:麻疯树萜醇I对家蚕无接触毒性,其急性毒性主要表现为胃毒作用,处理后48、72和120 h的LC50值分别为0.579、0.220和0.158 mg/mL。家蚕对麻疯树萜醇I处理 叶片的取食量显著少于对照组,24 h和 48 h的拒食中浓度(AFC50)分别为0.160和0.145 mg/mL。 取食麻疯树萜醇I后,家蚕体重增长显著被抑制,这一抑制作用具有明显的时间效应和浓度效应,即随着处理浓度的增高和处理时间的延长而逐渐增大。取食麻疯树萜醇I还导致家蚕中肠蛋白酶的比活力随时间逐渐下降,48 h时最低,0.25、0.125及0.062 5 mg/mL处理组蛋白酶比活力分别仅为对照的32.94%、43.35%、71.45%;处理浓度越大,蛋白酶比活力越低。石蜡切片显示,麻疯树萜醇I主要影响了中肠细胞的组织结构,引起细胞从基底膜上脱落,细胞破裂,使脂肪体消融等。表明麻疯树萜醇I对消化系统的破坏是其导致试虫中毒的重要机制之一。  相似文献   

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