对唑来膦酸衍生物1-羟基-2-(4-甲基-1H-咪唑-1-基)乙烷-1,1-双膦酸(M4IDP)进行99mTc标记,得到^99mTc-M4IDP,研究了其小鼠体内分布和兔骨显像性能。结果表明,在小鼠注射^99mTc-M4IDP60 min后,骨(7.85±0.73)%/g和关节(14.29±0.53)%/g摄取都达到最大值,肌肉(0.45±0.03)%/g和血(1.88±0.22)%/g的摄取很低。兔经注射^99mTc-M4IDP 1 h后即可获得清晰的骨显像,本底吸收很低。表明99mTc-M4IDP是一种软组织代谢速率快、骨吸收高的性能优异的新型骨显像剂。
The compound 1-Hydroxy-2-(4-methyl-lH-imidazoleyl)-ethylidene-l,l-bis- phosphonate (MflDP) was labeled by 99mTc to afford 99mTc-M41DP. The biodistribution in mice and bone image in rabbit for 99mTc-M4IDP were studied. The results showed that the uptakes of bone and jiont of 99mTc-M4IDP in mice reached the maximum of 7.85 ± O. 73 %/g and 14.29 ± 0.53 %/g respectively at 60 min post injection. It also had low uptake in muscle (0.45 ± 0.03 %/g) and blood (1.88 ± 0.22 %/g) , respectively. The clear bone image of rabbit was obtained at 1 h post injection of 99mTc-M4IDP. The perliminary investgation indicated that the 99mTc-M4IDP is an excellent bone imaging agent with rapid elimination in soft tissue and high uptake in bone.