Acidic and basic triamterene derivatives were evaluated with respect t
o their acute toxicity. After single intravenous application in mice,
derivatives with a basic side-chain were much more toxic than compound
s with an acidic side-chain. There is a significant correlation betwee
n the potassium retaining properties (measured as ED(50)) and the acut
e toxicity (measured as LD(50)) of the substances. The low acute toxic
ity after oral application of the compounds can be explained by their
low oral bioavailability.