HEDTMP (N-(2-hydroxyethyl) ethlenediamine-1,1,2-tri(methylene phosphonic acid)) was labeled with 153Sm. The formation condition, stability, rabbit bone imaging and mouse bio-distribution of 153Sm -HEDTMP were investig...HEDTMP (N-(2-hydroxyethyl) ethlenediamine-1,1,2-tri(methylene phosphonic acid)) was labeled with 153Sm. The formation condition, stability, rabbit bone imaging and mouse bio-distribution of 153Sm -HEDTMP were investigated. The results showed that weak basic media and high ligand’s concentration were favorable to form 153Sm-HEDTMP, and neutral or weak basic media increase the stability of 153Sm-HEDTMP. And the higher the con- centration of HEDTMP was, the more stable the labeling complex was. Bio-distribution study indicated the uptake of 153Sm-HEDTMP in skeleton was high ((25.68±1.22)ID%/g bone at 3 h post injection and (16.56±1.01)ID%/g bone at 48 h post injection), while the non-target tissue uptake and retention were relatively low, so 153Sm-HEDTMP is a promising bone tumor therapeutic agent.展开更多
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
TTHMP (triethylenetetraaminehexamethylenephosphonic acid) was labeled with 153Sm. The labeling condition, stability, mole ratio of 153Sm to TTHMP, rabbit bone imaging and bio-distribution of 153Sm-TTHMP in mice were i...TTHMP (triethylenetetraaminehexamethylenephosphonic acid) was labeled with 153Sm. The labeling condition, stability, mole ratio of 153Sm to TTHMP, rabbit bone imaging and bio-distribution of 153Sm-TTHMP in mice were investigated. The results showed that weak basic media and high concentration ligands were favorable to form 153Sm-TTHMP; labeling compounds were stable at pH 7 in 7 days. The results also indicated that the chemical mole ratio of 153Sm-TTHMP is n(153Sm)﹕n(TTHMP) = 1﹕1 and skeleton uptake of 153Sm-TTHMP is high((13.96(3.51)%/g at 1h post injection and (13.54(2.98)%/g at 48h post injection), while the non-target tissue uptake is relatively low, so 153Sm-TTHMP is a promising bone tumor therapeutic agent.展开更多
文摘HEDTMP (N-(2-hydroxyethyl) ethlenediamine-1,1,2-tri(methylene phosphonic acid)) was labeled with 153Sm. The formation condition, stability, rabbit bone imaging and mouse bio-distribution of 153Sm -HEDTMP were investigated. The results showed that weak basic media and high ligand’s concentration were favorable to form 153Sm-HEDTMP, and neutral or weak basic media increase the stability of 153Sm-HEDTMP. And the higher the con- centration of HEDTMP was, the more stable the labeling complex was. Bio-distribution study indicated the uptake of 153Sm-HEDTMP in skeleton was high ((25.68±1.22)ID%/g bone at 3 h post injection and (16.56±1.01)ID%/g bone at 48 h post injection), while the non-target tissue uptake and retention were relatively low, so 153Sm-HEDTMP is a promising bone tumor therapeutic agent.
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.
文摘TTHMP (triethylenetetraaminehexamethylenephosphonic acid) was labeled with 153Sm. The labeling condition, stability, mole ratio of 153Sm to TTHMP, rabbit bone imaging and bio-distribution of 153Sm-TTHMP in mice were investigated. The results showed that weak basic media and high concentration ligands were favorable to form 153Sm-TTHMP; labeling compounds were stable at pH 7 in 7 days. The results also indicated that the chemical mole ratio of 153Sm-TTHMP is n(153Sm)﹕n(TTHMP) = 1﹕1 and skeleton uptake of 153Sm-TTHMP is high((13.96(3.51)%/g at 1h post injection and (13.54(2.98)%/g at 48h post injection), while the non-target tissue uptake is relatively low, so 153Sm-TTHMP is a promising bone tumor therapeutic agent.
