Urinary excretion and metabolism of 4-ipomeanol was studied in rats injected ip with the radiolabeled compound. There was a rapid elimination of radioactivity in the urine, amounting to 47% of the administrated dose within 4hr. One major metabolite was isolated and purified by HPLC. Analysis by analytical HPLC, beta-glucuronidase hydrolysis, and mass spectrometry identified this material as ipo-meanol 4-glucuronide. The large amount of this metabolite excreted suggests that 4-glucuronidation is an important detoxication reaction in vivo for 4-ipomeanol in rats.