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신장기능영상용 방사성의약품 Bz - MAG3 ( Benzoylmercaptoacetylglycylglycylglycine ) 의 키트화 및 체내분포
고창순(Chang Soon Koh),이명철(Myung Chul Lee),정준기(June Key Chung),이동수(Dong Soo Lee),김영주(Young Ju Kim),정재민(Jae Min Jeong),장영수(Young Soo Chang),조정혁(Jung Hyuk Cho) 대한핵의학회 1996 핵의학 분자영상 Vol.30 No.3
N/A The MAG3 is a tubular excreting radiopharmaceutical for renal image. We synthe-sized benzoyl MAG3 (Bz-MAG3) and made a kit for labeling with Tc-99m. We checked the labeling effeciency of Tc-99m labeled MAG3 and biodistribution. Labeling efficiency was checked by TLC- SG (acetonitrile/H2O=2/1). After injecting of 1 mCi of Tc-99M-MAG3 to ICR-mice, Tmax(min), T1/2(min) were obtained in the renogram. Sequencial images (30sec, 2min, 5min, 10min, 15min, 20min) of TC-99m-MAG3 were compared with those of commercial Tc-99m-DTPA (Du Pont Merck Pharmaceutical Co.) kit. 1) The Rf value of synthesized Tc-99m-MAG3 was 0.78 and labeling efficiency was 97.5±1.9% (n=10). 2) The dynamic images of the Tc-99m-MAG3 were better than those of the Tc-99m-DTPA. 3) The Tmax(min.) and T1/2(min.) of Tc-99m-MAG3 (n=10) were 1.5±0.5 (left), 1.4±0.4(right), and 4.3±1.4 (left), 4.8±2.0 (right), respectivel. The Tmax(min.) and T1/2(min.) of Tc-99m-DTPA (n=7) were 2.7±1.6 (left), 2.7±1.6 right), and 3.8±1.7 (left), 4.5±2.7 (right), respectively. The quaility of image and labeling efficiency of the synthesized Bz-MAG3 kit were excellent, that it was supposed to be used in routine clinical work.
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Dione Bisoxime 계통의 화합물에 대한 테크네슘표지 원리에 관한 연구
고창순(Chang Soon Koh),이명철(Myung Chul Lee),정준기(June Key Chung),이동수(Dong Soo Lee),이경한(Kyung Han Lee),정재민(Jae Min Jeong),곽철은(Cheol Eun Kwark),오승준(Seung Joon Oh),정수욱(Soo Wook Chung),조정혁(Jung Hyuk Cho) 대한핵의학회 1995 핵의학 분자영상 Vol.29 No.1
N/A 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.
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담체가 Re-188-Hydroxyethylidene Diphosphonate의 표지와 생체내분포에 미치는 영향
장영수,이상은,이승진,이명철,이동수,정준기,정재민,조정혁,김보광,김인걸 대한핵의학회 2000 핵의학 분자영상 Vol.34 No.4
Purpose: Re-188-Hydroxyethylidene diphosphonate (HEDP) is a new cost-effective agent for systemic radioisotope therapy of metastatic bone pain. We investigated the influence of carrier for labeling and biodistribution of Re-188-HEDP using HEDP kit with or without carrier (KReO4). Materials and Methods: The kits (HEDP 15 mg, gentisic acid 4 mg and SnCl2.2H2O 4.5 mg) with or without carrier (KReO4 0.1 mg) were labeled with Re-188 solution, made available from an in-house generator by boiling for 15 min. We compared the labeling efficiency and stability of carrier-added and carrier-free preparations of Re-188-HEDP. Biodistribution and imaging studies of each preparation were performed in ICR mice (1.85∼3.7 MBq/0.1 ml) and SD rats (74.1∼85.2 MBq/0.5 ml). Results: The carrier-added preparation showed high labeling efficiency (95% at pH 5) and high stability in serum (88%, 3 hr). However, the carrier-free preparation showed low labeling efficiency (59% at pH 5) and low stability (43%, 3 hr). The carrier-added preration showed high uptake in bone and low uptake in stomach and kidneys. However, the carrier-free preparation showed lower uptake in bone and higher uptake in both stomach and kidneys, which is supposed to be due to released perrhenate. The carrier-added preparation also showed better images with higher skeletal accumulation, lower uptake in other organs and lower soft tissue uptake than the carrier-free preparation. Conclusion: The results of these studies clearly demonstrate that addition of carrier perrhenate is required for high labeling efficiency, stability, bone uptake and good image quality of Re-188-HEDP. (Korean J Nucl Med 2000;34:344-52)
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