Summary.-The antitumour agent 5-(3,3-dimethyl-1-triazeno)imidazole-4-carboxamide (DTIC) was found to inhibit competitively the low-Km cyclic AMP phosphodiesterase activity in an ammonium-sulphate-precipitable fraction of the 2,000g supernatant of rat liver. With substrate concentration at 0-25 [M, 150 was 790 /tM for DTIC and 350 tM for theophylline. DTIC at 2 mm more than doubled the cAMP response to glucagon in hepatocytes and to adrenaline in MH1Cj hepatoma cells, indicating that it also exerts its inhibitory effect on the phosphodiesterase in intact cells. The possible contribution of the phosphodiesterase inhibition to the growthinhibitory and cytotoxic effects of DTIC is discussed.