TCTMP ( 1,4,8,11-tetraaza cyclotetradecyl- 1,4,8,11-tetramethylene phosphonate) was synthesized and coupled with 188Re. The 188Re-TCTMP's coupling condition, stability and bio-distribution in mice were investigate...TCTMP ( 1,4,8,11-tetraaza cyclotetradecyl- 1,4,8,11-tetramethylene phosphonate) was synthesized and coupled with 188Re. The 188Re-TCTMP's coupling condition, stability and bio-distribution in mice were investigated.The results showed that satisfactory yield of 188Re could be obtained under the conditions of media pH=2.0, 0.8～1.6 mg of SnCl2 and 50 mg of ligand. 188Re-TCTMP was stable (complexation yield ＞95%) in 8 d without protection of N2. The result of bio-distribution indicated that 188Re-TCTMP had a strong affinity to skeleton and very low non-target tissue's uptake, and the amount of 188Re-TCTMP in blood was (0.06±0.02)%ID/g 6 h after injection,whereas the concentration of 188Re-HEDP (1-hydroxy-ethylidene diphosphonate) in blood was (0.28±0.05)%ID/g 6 hafter injection. Compared with 188Re-HEDP, 188Re-TCTMP exhibits better potential for the treatment of metastases.展开更多
文摘TCTMP ( 1,4,8,11-tetraaza cyclotetradecyl- 1,4,8,11-tetramethylene phosphonate) was synthesized and coupled with 188Re. The 188Re-TCTMP's coupling condition, stability and bio-distribution in mice were investigated.The results showed that satisfactory yield of 188Re could be obtained under the conditions of media pH=2.0, 0.8～1.6 mg of SnCl2 and 50 mg of ligand. 188Re-TCTMP was stable (complexation yield ＞95%) in 8 d without protection of N2. The result of bio-distribution indicated that 188Re-TCTMP had a strong affinity to skeleton and very low non-target tissue's uptake, and the amount of 188Re-TCTMP in blood was (0.06±0.02)%ID/g 6 h after injection,whereas the concentration of 188Re-HEDP (1-hydroxy-ethylidene diphosphonate) in blood was (0.28±0.05)%ID/g 6 hafter injection. Compared with 188Re-HEDP, 188Re-TCTMP exhibits better potential for the treatment of metastases.
