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The biodistribution of 125I-BMIPP and the variation of myocardial uptake of 125I-BMIPP using themetabolic intervention drug were reported. Myocardial uptake of the 125I-BMIPP in rats showed a peak of 5.70ID%/gat 2 min. The ratios of myocardium to blood, to liver and to lung at 30 min were 3.40, 2.64 and 2.88 respectively. Theinitial elimination half time of 4.0 min in rabbits was in accordance with the half elimination time of free fatty acidfrom 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 constantlevel of activation up to 2 h. Partition coefficients (lgP) were 1.93 and 1.68, respectively.