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1. After intravenous administration of [¹⁴C]histamine in rabbits, the urinary excretion of [¹⁴C]histamine and [¹⁴C]histamine metabolites was examined over a period of 4 hr.

2. It was found that [¹⁴C]histamine was excreted in the unchanged form only in small amounts (6-7%), while 54-71% was eliminated in the form of its metabolites.

3. Under normal conditions, the percentage excretion of metabolites, but not of histamine, showed a dose dependence. With the higher [¹⁴C]histamine dose, a significantly smaller proportion of the dose given was excreted as metabolites than with the lower dose. The proportion of unchanged [¹⁴C]histamine excreted remained constant.

4. Pre-treatment with histamine infusions, or with mepyramine maleate, caused an increase in the excretion of [¹⁴C]histamine metabolites while the excretion of [¹⁴C]histamine remained unchanged.

5. Pre-treatment with a diuretic, a combination of mersalyl and theophylline, did not influence the excretion of [¹⁴C]histamine nor of its metabolites.