Possible Anxiolytic Effects of Ivermectin in Rats

Ivermectin, a mixture of 22,23-dihydroavermectin B_1a (80%) and B_1b (20%), is produced by Streptomyces avermectilis, an actinomycete. It is a macrocyclic lactone disaccharide, a member of the avermectin family, and is used as an antiparasitic drug. Previous studies performed in our laboratory showed that doramectin, another avermectin drug, interferes with GABAergic-related behaviours, leading to anxiety and seizures. The objective of the present study was to examine the effects of ivermectin (0.5 and 1.0 mg/kg) on the central nervous system of rats, using behavioural models related to GABAergic neurotransmission. A known anxiolytic drug, diazepam, was used as a positive control. Open field and elevated plus-maze behaviours, as well as conflict behaviour to a conditioned response, were assessed. The effects of ivermectin and diazepam in reversing the anxiety induced by picrotoxin was studied. The protective effects of ivermectin on pentylenetetrazole- and picrotoxin-induced seizures were also investigated. In the open field, 1.0 mg/kg ivermectin decreased locomotion frequency at 15 and 60 min of observation, rearing behaviour showed a biphasic effect at 15 and 30 min and duration of immobility was increased in all sessions after 1.0 mg/kg ivermectin. These data suggest anxiolytic or sedative effects. Ivermectin and diazepam both had a tendency to cause an increase both in the number of entries into the open arms and on the time spent in the open arms of an elevated plus-maze. Picrotoxin on its own reduced the number of entries as well as the time spent in the open arms. Both diazepam and ivermectin reversed these effects of picrotoxin. In conflict behaviour analysis, ivermectin and diazepam gave the classic effect of an anxiolytic drug, reversing the conditioned response to shock. Ivermectin protected rats from the convulsant effects of pentylenetetrazole but not from those of picrotoxin. Thus, ivermectin had the pharmacological profile of an anxiolytic drug with GABAergic properties. The lack of effect on seizures induced by picrotoxin suggests that the action of ivermectin is different from that of the benzodiazepine drugs.     

Avermectins,a novel class of compounds: implications for use in arthropod pest control

对阿维菌素B_2a进行结构优化,在阿维菌素B_2a的C4\     

山东省植物根结线虫鉴定、危害植物种类及药剂敏感性检测

调查了山东省根结线虫的危害植物种类,以危害较重的4个不同用药水平地区的蔬菜根结线虫为研究对象,进行了形态学和酯酶同工酶谱鉴定,采用室内接触法和室内盆栽试验测定和比较了不同种群2龄幼虫对阿维菌素和辛硫磷的敏感性,并比较了保护酶的差异。山东省保护地蔬菜根结线虫为南方根结线虫Meloidogyne incognita,其危害的植物有51种,占调查总数的66.2%。2龄幼虫对阿维菌素的敏感性差异倍数为0.97～1.23、对辛硫磷为0.94～1.10,无显著性差异,其总体趋势为用药历史越长、用药量越多,药剂的敏感性越低;雌虫体内的可溶性蛋白存在细微差异,而POD和SOD同工酶谱带无显著差异。     

阿维菌素对蛋鸡皮刺螨的驱杀试验

用蛋鸡为试验动物,将伊维菌素预混剂按1mg/kg饲料的浓度混入饲料为对照药物,检测1.25,1.00,0.75mg/kg饲料的阿维菌素预混剂和400mg/kg体重的阿维菌素粉剂(分两次)对鸡皮刺螨的驱杀效果。结果表明:阿维菌素预混剂能驱杀鸡皮刺螨,与伊维菌素预混剂驱杀鸡皮刺螨的效果一致,而阿维菌素粉剂驱杀鸡皮刺螨的效果不如阿维菌素预混剂。阿维菌素预混剂和阿维菌素粉剂都能显著增加料蛋比,提高饲料转化率。     

杀虫抗生素的研究进展

杀虫抗生素是一种生物源杀虫剂,具有高效、低毒、对环境无公害等特点,在病虫害综合防治中占据重要的地位.介绍了目前杀虫抗生素的应用及研究现状,列举了几种研究成功的杀虫抗生素,并对杀虫抗生素的研究前景作了展望.     

三种兽药在不同暴露系统对蚯蚓的急性毒性

采用人工土壤法和滤纸法对不同浓度的阿维菌素、安普霉素、磺胺二甲基嘧啶3种常用兽药对蚯蚓的急性毒性进行了研究。结果表明,用土壤法和滤纸法测定的阿维菌素对蚯蚓的半数致死浓度(LC50)分别为17.06mg·kg-1和4.63×10-3mg·cm-2,阿维菌素对蚯蚓具有一定的毒性作用,其皮肤接触毒性比土壤食入毒性更大。用滤纸法测定的安普霉素、磺胺二甲基嘧啶对蚯蚓的半数致死浓度(LC50)分别大于10mg·cm-2和15mg·cm-2;用土壤法测定安普霉素、磺胺二甲基嘧啶对蚯蚓的半数致死浓度(LC50)均大于5000mg·kg-1,表明安普霉素、磺胺二甲基嘧啶对蚯蚓的毒性较低。     

阿维菌素与氰戊菊酯复配对桃蚜的增效作用

阿维菌素与氰戊菊酯的各种配比均对桃蚜存在着不同程度的增效作用 ,其中以阿维菌素与氰戊菊酯按有效成分 1∶2 4的比例复配增效作用最为明显 ,共毒系数达到 2 97.84。室内药效试验也表明 ,2 0 %混剂乳油(0 .8%阿维菌素 19.2 %氰戊菊酯 )的药效明显高于 2 0 %氰戊菊酯乳油 ,与 0 .9%阿维菌素乳油相当     

线粒体损伤在阿维菌素致体外培养神经细胞凋亡中的作用

通过体外培养王鸽脑神经细胞，并按终浓度0、2．5、5和10μg／L阿维菌素（AVM）染毒，培养24h时，经透射电镜观察神经细胞超微结构，DNA断裂评价细胞凋亡，MTT法测定线粒体活性，酶标仪检测Caspase-3、Caspase-9活性，流式细胞术测定线粒体跨膜电位（△ψm），探讨线粒体损伤在AVM致体外培养神经细胞凋亡中的作用。结果显示，AVM可明显抑制神经细胞线粒体的活性，引起△ψm下降，Caspase-3和Caspase-9活性升高，神经细胞发生凋亡，存在明显的剂量效应关系。证实，线粒体损伤是AVM致体外培养神经细胞凋亡的机理之一。     

Evaluation of neonicotinoid, organophosphate and avermectin trunk injections for the management of avocado thrips in California avocado groves

BACKGROUND: Trunk injections of systemic insecticides were evaluated for the management of avocado thrips. Insecticide residues were quantified in leaves to determine when after treatment, and for how long, toxic concentrations of the insecticides were present. Residues in fruit were quantified to determine whether trunk injection of insecticides might present a greater risk than traditional application methods for contaminating fruit. RESULTS: Residues of imidacloprid and dinotefuran were at least tenfold higher in leaves when trees were treated via trunk injection compared with soil application. Dinotefuran uptake was more rapid than imidacloprid, and no residues were detected within fruit. Acephate was also mobilized very rapidly and gave good control of thrips in bioassays; however, residues of acephate and its insecticidal metabolite methamidophos were detected in the fruit for up to 4 weeks after injection. Avermectin uptake was very slow, and it was ineffective against avocado thrips. CONCLUSIONS: Trunk injections of acephate and dinotefuran permitted rapid uptake into avocados, and they are strong candidates as control methods for avocado thrips. However, residues of organophosphates in fruit could necessitate increased preharvest intervals. Residues of neonicotinoids were below detection limits in fruit, suggesting that neonicotinoids may be the more suitable control option of the two chemical classes. Copyright © 2012 Society of Chemical Industry