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

Phenylpyrazoles 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^?5 M 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^?5 M). At 10^?6 M 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 in intact animals.