Myocardial uptake of 125I-IPPA in rats showed a peak of 4.4% of injected dose per gram. The half elimination time of myocardium was 3.8 min and the maximal uptake of thyroid is only 0.005%ID/organ at 120min. The initi...Myocardial uptake of 125I-IPPA in rats showed a peak of 4.4% of injected dose per gram. The half elimination time of myocardium was 3.8 min and the maximal uptake of thyroid is only 0.005%ID/organ at 120min. The initial half time of 2.7 min in rabbits was obtained from the elimination curve of radioactivity in blood. In vitro binding test for 125I-IPPA to HSA showed rather constant level of activation during two hours. The second peak of extraction was observed in major organs of rats, in rabbits’ elimination of radioactivity and in binding test for 125I-IPPA to albumin in vivo. Toxicity trial was up to standard. The tolerance of a mouse to IPPA was 560 times as high as that of a person to IPPA. It demonstrated that 125I-IPPA could be quickly extracted by myocardium, and its catabolites were excreted in the urine with almost no iodine loss. All the results were found to agree with the expectations based on the principal metabolic path of phenyl fatty acid.展开更多
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
A new method for tile preparation of p-iodophenyl pentadecanoic acid (IPPA)has been developed. The synthesis are described, and physical properties of IPPA are characterized by IR, 1HNMR, elementary analysis and MS. 1...A new method for tile preparation of p-iodophenyl pentadecanoic acid (IPPA)has been developed. The synthesis are described, and physical properties of IPPA are characterized by IR, 1HNMR, elementary analysis and MS. 125I-IPPA can be easily prepared bytwo methods: direct labeling and solid-phase iodo-exchange labeling, and the yields of labelingare 80% and 65%, respectively. The radiochcnrical purities are higher than 98% after beingextracted with chloroform and he-cane.展开更多
基金Natural Science Foundation of Jiangsu Province!(BK97185) Science Foundation of Health Department of Jiangsu Province!(H9535)
文摘Myocardial uptake of 125I-IPPA in rats showed a peak of 4.4% of injected dose per gram. The half elimination time of myocardium was 3.8 min and the maximal uptake of thyroid is only 0.005%ID/organ at 120min. The initial half time of 2.7 min in rabbits was obtained from the elimination curve of radioactivity in blood. In vitro binding test for 125I-IPPA to HSA showed rather constant level of activation during two hours. The second peak of extraction was observed in major organs of rats, in rabbits’ elimination of radioactivity and in binding test for 125I-IPPA to albumin in vivo. Toxicity trial was up to standard. The tolerance of a mouse to IPPA was 560 times as high as that of a person to IPPA. It demonstrated that 125I-IPPA could be quickly extracted by myocardium, and its catabolites were excreted in the urine with almost no iodine loss. All the results were found to agree with the expectations based on the principal metabolic path of phenyl fatty acid.
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.
文摘A new method for tile preparation of p-iodophenyl pentadecanoic acid (IPPA)has been developed. The synthesis are described, and physical properties of IPPA are characterized by IR, 1HNMR, elementary analysis and MS. 125I-IPPA can be easily prepared bytwo methods: direct labeling and solid-phase iodo-exchange labeling, and the yields of labelingare 80% and 65%, respectively. The radiochcnrical purities are higher than 98% after beingextracted with chloroform and he-cane.
