A novel [99mTc[triple bond]N]2+ complex of metronidazole xanthate as a potential agent for targeting hypoxia |
| |
Authors: | Mallia Madhava B Mathur Anupam Subramanian Suresh Banerjee Sharmila Sarma H D Venkatesh Meera |
| |
Institution: | Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Mumbai, India. |
| |
Abstract: | A xanthate derivative (L) at the pendant hydroxy group of metronidazole, a nitroimidazole known to possess affinity for hypoxic tumors, has been used as the carrier molecule for targeted delivery of the gamma-emitting radioisotope 99mTc to tumors. The xanthate residues (S2(-)) from two molecules of this ligand (L) were used for chelation with the 99mTcN]2+ intermediate to form a square pyramidal and neutral 99mTcN/L2] complex in >95% yield using a low ligand concentration of 1 mg/mL (approximately 3 x 10(-3) M). Biodistribution studies carried out in Swiss mice bearing fibrosarcoma tumor showed selective accumulation of the injected activity in the tumor (1.44 +/- 0.26% per gram 1 h pi) with major clearance through hepatobiliary route. The complex showed high tumor/muscle ratio (2.15 and 3.35 at 1 and 3 h post-injection, respectively) and tumor/blood ratio, which were comparable to hypoxia targeting agents 99mTc-BMS181321 and 99mTc-BRU59-21 reported earlier. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|