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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 pro- tection of N2. The result of bio-distribution indicated that188Re-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 h after injection. Compared with 188 Re-HEDP, 188Re-TCTMP exhibits better potential for the treatment of metastases.
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 the yield yield of 188 Re 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 days without pro- tection N2. The result of bio-distribution indicated that 188Re-TCTMP had a strong affinity to skeleton and very low non-target tissue uptake, and the amount of 188Re-TCTMP in blood was (0.06 ± 0.02)% ID / g 6 h after injection , the concentration of 188Re-HEDP (1-hydroxy-ethylidene diphosphonate) in blood was (0.28 ± 0.05)% ID / g for 6 h after injection. Compared with 188 Re-HEDP, 188Re-TCTMP exhibits better potential for the treatment of metastases.