• The Korean Journal of Nuclear Medicine
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• v.35 no.1
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• pp.69-74
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• 2001

Purpose: $^{99m}Tc$-HMPAO is a radiopharmaceutical for imaging cerebral blood flow. HMPAO (RR, SS)-4.8-diaza-3,6,6,9-tetramethylundecan-2,10- dione bisoxime) has three stereoismers such as, meso-. d-, and l-HMPAO. Techentium complexes of meso-HMPAO and d,l-HMPAO are known to have different in vivo brain uptakes. In this study, enantiomers of HMPAO (d-HMPAO and l-HMPAO) were separated from d,l-HMPAO. These enantiomers were labeled with $^{99m}Tc$ and the biodistribution studies were performed in mice. Materials and Methods: An intermediate imine product was produced from 2,3-butanedione monooxime and 2,2-dimethyl-1,3-propanediamine (54% yield) and was reduced into a mixture of three isomers (35% yield). The meso-isomer was separated from d,l-mixture by repeated fractional crystallization (11 % yield). The d- and l-enantiomers were subsequently separated by co-crystallization with optical isomers of tartaric acid (25% and 5% yield. respectively). Each enantiomeric HMPAO was labeled with $^{99m}Tc$ by reacting with $SnCI_2{\cdot}2H_2O\;and\;^{99m}Tc$-pertechnetate. Biodistribution study was performed 1 hr after tail vein injection to ICR mice. Results: Radiochemical purities of each compound were over 80%. In biodistribution study. the brain uptakes of d,l- d- and l-form were 1.34, 1.12 and 1.67% ID/g, respectively. In case of l-lsomer the brain uptake was higher (1.5 fold) than d-isomer. Conclusion: We successfully purified each enantiomeric HMPAO. In biodistribution study of stereoismers of $^{99m}Tc$-HMPAO in mice, l-HMPAO may show better brain image than d,l-HMPAO which was supplied in a commercial kit.

• The Korean Journal of Nuclear Medicine
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• v.30 no.3
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• pp.367-371
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• 1996

The $MAG_3$ is a tubular excreting radiopharmaceutical for renal image. We synthesized benzoyl $MAG_3\;(Bz-MAG_3)$ and made a kit for labeling with $^{99m}Tc$. We checked the labeling efficieny of $^{99m}Tc$ labeled $MAG_3$ and biodistribution. Labeling efficieny was checked by TLC-SG (acetonitrile/$H_2O$=2/1). After injecting of 1 mCi of $^{99m}Tc-MAG_3$ to ICR-mice, $T_{max}(min),\;T_{1/2}(min)$ were obtained in the renogram. Sequential images (30sec, 2min, 5min, 10min, 15min, 20min) of $^{99m}Tc-MAG_3$ were compared with those of commercial $^{99m}Tc$-DTPA (Du Pont Merck Pharmaceutical Co.) kit. 1) The $R_f$ value of synthesized $^{99m}Tc-MAG_3$ was 0.78 and labeling efficiency was $97.5{\pm}1.9%$ (n=10). 2) The dynamic images of the $^{99m}Tc-MAG_3$ were better than those of the $^{99m}Tc$-DTPA. 3) The $T_{max}(min.)$ and $T_{1/2}(min.)$ of $^{99m}Tc-MAG_3$ (n=10) were $1.5{\pm}0.5$ (left), $1.4{\pm}0.4$ (right), and $4.3{\pm}1.4$ (left), $4.8{\pm}2.0$ (right), respectively. The $T_{max}(min.)$ and $T_{1/2}(min.)$ of $^{99m}Tc$-DTPA (n=7) were $2.7{\pm}1.6$ (left), $2.7{\pm}1.6$ (right), and $3.8{\pm}1.7$ (left), $4.5{\pm}2.7$ (right), respectively. The quaility of image and labeling efficiency of the synthesized $Bz-MAG_3$ kit were excellent, that it was supposed to be used in routine clinical work.