Pesticides are now recognised to interact with drug transporters, but only few data are available on this issue for carbamate pesticides, a widely used class of agrochemicals, to which humans are highly exposed. The present study was therefore designed to determine whether four representative carbamate pesticides, i.e. the insecticides aminocarb and carbofuran, the herbicide chlorpropham and the fungicide propamocarb, may impair activities of main drug transporters implicated in pharmacokinetics.

The interactions of carbamates with solute carrier and ATP-binding cassette transporters were investigated using cultured transporter-overexpressing cells, reference substrates and spectrofluorimetry-, liquid chomatography/tandem mass spectrometry- or radioactivity-based methods.

Aminocarb and carbofuran exerted no or minimal effects on transporter activities, whereas chlorpropham inhibited BCRP and OAT3 activities and propamocarb decreased those of OCT1 and OCT2, but cis-stimulated that of MATE2-K. Such alterations of transporters however required chlorpropham/propamocarb concentrations in the 5–50 µM range, likely not relevant to environmental exposure. Trans-stimulation assays and propamocarb accumulation experiments additionally suggested that propamocarb is not a substrate for OCT1, OCT2 and MATE2-K.

These data indicate that some carbamate pesticides can interact in vitro with some drug transporters, but only when used at concentrations higher than those expected to occur in environmentally exposed humans.

现在人们认识到农药与药物转运蛋白发生相互作用，但关于氨基甲酸酯农药（人类广泛接触的一种广泛使用的农用化学品），只有很少的数据可用于此问题。因此，本研究旨在确定四种代表性的氨基甲酸酯农药，即杀虫剂氨基碳和呋喃丹，除草剂氯丙胺和杀真菌剂丙氨威是否可能损害与药代动力学有关的主要药物转运蛋白的活性。

氨基甲酸酯与溶质载体和ATP结合盒转运蛋白的相互作用使用培养的转运蛋白过表达细胞，参比底物和基于荧光光谱法，液相色谱/串联质谱法或放射性的方法进行了研究。

氨基碳水化合物和呋喃丹对转运蛋白的活性没有影响或影响很小，而氯丙胺抑制了BCRP和OAT3的活性，丙草胺降低了OCT1和OCT2的活性，但顺式刺激了MATE2-K。然而，这种转运蛋白的改变要求氯丙胺/丙草威的浓度在5-50 µM范围内，这可能与环境暴露无关。反式刺激试验和丙草威的积累实验还表明，丙草威不是OCT1，OCT2和MATE2-K的底物。

这些数据表明，某些氨基甲酸酯农药可以在体外与某些药物转运蛋白发生相互作用，但仅当其浓度高于环境暴露的人类所预期的浓度时才可以。