Abstract
Effects of Cl<sup>–</sup> channel blockers and antimalarial drugs on the Ca<sup>2+</sup>-dependent Cl<sup>–</sup> current in <i>Xenopus</i> oocytes were studied using a two-microelectrode voltage-clamp technique. Chloride channel blockers, such as stilbene disulfonic acids and carboxylic acids, inhibit the Cl<sup>-</sup> current in oocytes. The calculated half-inhibitory concentrations (IC<sub>50</sub>) of these blockers on the oocyte Cl<sup>–</sup> current demonstrate an order of potency of 4,4’-diisothiocyanatostilbene-2,2’-disulfonic acid > anthracene-9-carboxylic acid > diphenylamine-2-carboxylic acid > indanyloxyacetic acid. This is different from the potency observed in the outwardly rectifying Cl<sup>-</sup> channels of epithelial cells. The blocking effect of these Cl<sup>–</sup> channel blockers on the Ca<sup>2+</sup>-dependent Cl<sup>–</sup> current in oocytes was observed to be stronger at positive membrane potentials. In addition, various antimalarial drugs, such as quinine’s derivatives and artesunate, inhibit the Ca<sup>2+</sup>-dependent Cl<sup>–</sup> current in oocytes. These inhibitory effects on cytoplasmic membrane Cl<sup>–</sup> channels may be responsible for the pharmacological action and toxic side effects of these compounds.
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