Dione Bisoxime 계통의 화합물에 대한 테크네슘표지 원리에 관한 연구 = Tc - 99m Labeling of Dione Bisoxime Compounds

다국어 초록 (Multilingual Abstract)

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다국어 초록 (Multilingual Abstract)

Tc-99m Labeled hexamethylenepropyleneamineoxime ([Tc-99m-HAMPAO) is a famous amine -oxime compound and is widely used to construct SPECT images of cerebral blood flow. To investigate the relationship between chemical structure and radiolabeling in these kind of diamine -oxime compounds, we synthesized seven compounds by Schiff's base formation and successive reduction with sodium borohydride. They wese (RR/SS)-4,8-diaza-3,6,6,9-tetramethylundecane- 2,10-dione bisoxime (2), (RR/SS/meso)-4,8-diaza-3,9-dimethy-lundecane-2,10-dione bisoxime (4), (RR/SS/meso)-4,8-diaza-3,10-dimethyldodecane-2,11-dione bisoxime (6), (RR/SS/meso)-4,7-diaza- 3,6,6,8-tetramethyldecane-2,9-dione bisoxime (8), (RR/SS/meso)-4,7-diaza-5,6-cyclohexyl-3,8-dime- thyldecane-2,9-dione bisoxime(10),(RR/SS/meso)-3,4-bis (l-aza-2-methyl-3-oxime-l-butyl)-benzoic acid (12), and (RR/SS/meso)-2,3-bis(1-aza-2-methyl-3-oxime-l-butyl) benzophenone (14). Chem- ical structures of al1 the synthesized compounds were identified by taking 1H spectrum. Among them, 2 and 4 are propyleneamine oxime(PnAO), 6 is butyleneamine oxime(BnAO) and 8, 10, 12 and 14 are ethyleneamine oxime (EnAO), Each compound (0.5 mg) was incubated with stannous chloride(0.5 g - 8 g), carbonate-bicarbonate buffer (final concentration = 0.1 M, pH7 - pH 10 ) and Tc-9mm- pertechenate ( 1 ml). Tc-99m labeling of these compounds were checked by ITLC (acetone), ITLC (normal saline), reverse phase TLC (50% acetonitrile) and ITLC (ethyl acetate). According to the results, EnAO's were not labeled by Tc-99m in any of above condition. About 11 % of maximum labeling efficiency was obtained with BnAO. However, 4 (PnAO) was labeled with Tc-99m to 85 % which is similar to the labeling efficiency of 2 (HMPAO). Hydrophilic impurity (9 %) was the most significant problem with the labeling of 4, however, pertechnetate (3 %) and colloid (3 %) were minor problem. In conclusion, we synthesized seven diamine bisoxime compounds, Among them, four EnAO compounds were not labeled by Tc-99m. A BnAO was labeled poor.