A method with several steps superior to literature has been developed for the preparation of B-methyl p-iodophenyl pentadecanoic acid(BMIPP). The synthesis and physical properties of BMIPP are described. It is charact...A method with several steps superior to literature has been developed for the preparation of B-methyl p-iodophenyl pentadecanoic acid(BMIPP). The synthesis and physical properties of BMIPP are described. It is characterized by IR, 1HNMR, elemental analysis and MS. 125I-BMIPP can be prepared by three methods: direct labeling, solid-state transfer labeling and Cu(I ) assisted labeling. Cu(I) assisted labeling is simple and not necessary to purify before clinical use. It can fulfil the requirements for kit labeling.展开更多
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 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.展开更多
基金Supported by Natural Science Foundation of Jiangsu Province (BK97185)
文摘A method with several steps superior to literature has been developed for the preparation of B-methyl p-iodophenyl pentadecanoic acid(BMIPP). The synthesis and physical properties of BMIPP are described. It is characterized by IR, 1HNMR, elemental analysis and MS. 125I-BMIPP can be prepared by three methods: direct labeling, solid-state transfer labeling and Cu(I ) assisted labeling. Cu(I) assisted labeling is simple and not necessary to purify before clinical use. It can fulfil the requirements for kit labeling.
基金Natural Science Foundation of Jiangsu Province(No.97185)by Department of Health of Jiangsu Province(No.H9508)
文摘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.
