Studies on Preparation of $^{131}I$ Labelled m-Iodobenzylguanidine $(^{131}I-MIBG)$ for Adrenomedullary Imaging

부신수실 영상용 $^{131}I$ 표지 메타요오도벤질구아니딘 $(^{131}I-MIBC)$의 제조에 관한 연구

To develop $^{131}I-labelled$ m-iodobeneylguanidine $(^{131}I-MIBG)$, various experiments such as synthesis of MIBG, establishment of labelling conditions, determination of radiochemical purity, and examination of stability were carried out. 1) m-Iodobenzylguanidine (MIBG) sulfate was synthesized with a total yield of 62.4% by the condensation of m-iodobenzylamine hydrochloride with cyanamide via MIBG bicarbonate. Its physical properties, IR, $^1H-NMR$, and elemental analysis data were nearly identical to those of literature. 2) Freeze-dried or vacuum-dried kit vials were prepared from the mixture so as to contain MIBG (2 mg), ascorbic acid (10 mg), copper (II) sulfate (0.14 mg), and tin (II) sulfate (0.5 mg) per vial. Copper ( I ) catalyzed radioiodination of MIBG was carried out using kit vials and 0.01 M $H_2SO_4$ as solvent at $100^{\circ}C$ for 30 min under nitrogen atmosphere (optimal conditions). Labelling yield was 98% and radiochemical purity was 99.5%, respectively. 3) Solid-phase radioiodination of MIBG was carried out at $155^{\circ}C$ for 30 min using the prepared vials to contain MIBG (2 mg) and ammonium sulfate (10 mg). Duplicate reactions under the same conditions showed labelling yield of 95% and radiochemical purity of 99.5%. 4) $^{131}I-MIBG$ prepared either by catalytic or by solid-phase exchange method showed radio-chemical purity of 99% even after 3 days storing at room temperature.