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Acidic and basic triamterene derivatives were evaluated with respect to their acute toxicity. After single intravenous application in mice, derivatives with a basic side-chain were much more toxic than compounds with an acidic side-chain. There is a significant correlation between the potassium retaining properties (measured as ED50) and the acute toxicity (measured as LD50) of the substances. The low acute toxicity after oral application of the compounds can be explained by their low oral bioavailability.
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