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Phenylpyrazoles, a new class of pesticide: Effects on neuromuscular transmission and acetylcholine responses

机译:苯基吡唑类新型杀虫剂:对神经肌肉传递和乙酰胆碱反应的影响

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AbstractPhenylpyrazoles constitute a newly developed class of chemicals with insecticidal and herbicidal properties. In acute toxicity experiments in rats, near‐lethal doses of phenylpyrazoles produce neurotoxic symptoms with an unknown mode of action. We have investigated the effects of two phenylpyrazoles, SLA4722 and SLA4685, in the frog neuromuscular junction and in the clonal muscle cell line BC3H‐1. In the frog neuromuscular junction SLA4722 at concentrations ⩾ 10−5M caused a pronounced increase in the frequency of miniature endplate potentials (MEPPs). SLA4685 caused a similar increase but was less potent. In the clonal muscle cell line BC3H‐1, SLA4685 produced a concentration‐dependent block of the acetylcholine (ACh) response (IC50= 2.4(±0.3) × 10−5M). At 10−6M a slight potentiating effect of SLA4685 on the ACh response was observed. SLA4722 was less potent in this preparation. The increased transmitter release might, at least partly, be responsible for the excitatory effects of the phenylpyrazoles
机译:摘要苯基吡唑类是一类新开发的具有杀虫和除草性能的化学品。在大鼠的急性毒性实验中,接近致死剂量的苯吡唑会产生神经毒性症状,其作用方式未知。我们研究了两种苯基吡唑(SLA4722 和 SLA4685)对青蛙神经肌肉接头和克隆肌肉细胞系 BC3H-1 的影响。在青蛙神经肌肉接头中,浓度⩾10−5M的SLA4722导致微型终板电位(MEPP)频率显着增加。SLA4685引起了类似的增加,但效力较小。在克隆肌细胞系BC3H-1中,SLA4685产生了乙酰胆碱(ACh)反应的浓度依赖性阻滞(IC50= 2.4(±0.3)×10−5M)。在10−6M时,观察到SLA4685对ACh反应的轻微增强作用。SLA4722在这种制剂中效力较弱。递质释放的增加可能至少部分是苯吡唑兴奋作用的原因

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