Synthesis and Application of Carborane Containing MR Imaging Agent

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In order to improve and optimize efficient neutron capture therapy (NCT) treatment, it is necessary to follow the distribution of a carrier in the body in real time. However, it has been difficult to estimate the boron content of the tumor using technologies available. We succeeded to synthesize the carborane containing gadolinium-dimethylenetriamine pentaacetic acid (DTPA) unit which is commercially available under the trade name of Magnevist and is used as an MR imaging contrast medium. The evaluation of the Gd-carborane complex as an MR imaging and boron carrier agent was carried out in vivo using tumor-bearing Donryu rats by means of MRI, ICP-AES, and α-autoradiography. The MR imaging revealed that the carborane Gd-DTPA was metabolized slower in the body in comparison with Gd-DTPA. The results of ICP-AES method indicated that compound was incorporated into normal tissues and metabolized quickly, whereas it was not accumulated into tumor and brain tissue. The α-autoradiography showed that a high level of boron was obtained in the internal organs and in the necrosis of tumor tissue.