PREPARATION AND BIODISTRIBUTION OF ~(188)Re-TCTMP

TCTMP(1,4,8,11tertraaza cyclotetradecyl1,4,8,11tetramethylene phosphonate) is synthesized and coupled with 188Re. The coupling condition,stability and biodistribution of 188ReTCTMP in mice are investigated. The results show that satisfactory complexation yield of 188Re could be obtained under condition of medium pH=2.0,0.8～1.6 mg of SnCl2 and 50 mg of ligand. The complex exhibits high stability and maintains its high complexation yield (>95%) in 8 d without protection of N2. The results of biodistribution indicate considerably strong affinity of 188ReTCTMP to bone and very low nontarget tissue's uptake. The concentration of 188ReTCTMP in blood is (0.06±0.02)%/g at 6 h after injection,while the concentration of 188ReHEDP is (0.28±0.05) %/g at 6 h after injection,which might be due to the higher stability of 188ReTCTMP in vitro and in vivo. Comparing with 188ReHEDP,188ReTCTMP exhibits better potential for the treatment of metastases.