The biodistribution of ¹²⁵I-BMIPP and the variation of myocardial uptake of ¹²⁵I-BMIPP using the metabolic intervention drug were reported. Myocardial uptake of the ¹²⁵I-BMIPP in rats showed a peak of 5.70ID%/g at 2 min. The ratios of myocardium to blood, to liver and to lung at 30min were 3.40, 2.64 and 2.88 respectively. The initial elimination half time of 4.0min in rabbits was in accordance with the half elimination time of free fatty acid from blood. Myocardial uptake of ¹²⁵I-BMIPP in the group of glucose-insulin was significantly increased (p<0.05) than those of the normal control. In vivo and in vitro binding test for ¹²⁵I-BMIPP to HSA showed a rather constant level of activation up to 2h. Partition coefficients (lgp) were 1.93 and 1.68, respectively.