Synthesis of Tc-D,D-HMPAO and Tc-L,L-HMPAO and their comparison of chemical and biological properties

Tc- d,d- and Tc- l,l-HMPAO were synthesized. The stability of Tc- d,d- and Tc- l,l-HMPAO in vitro is similar to that of d,l-isomers by the spectrophotometric and three strips methods. Cerebral uptake (%D in brain) for the l,l-isomer is higer than the d,d- and d,l-isomer in rats. Delayed studies show...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1999-11, Vol.9 (22), p.3199-3202
Main Authors: Ding, Hueisch-Jy, Huang, Ying-Fong, Tzeng, Cherng-Chyi, Wei, Li-Mei, Yeh, Si-Jung
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Contrast media. Radiopharmaceuticals
Female
Isomerism
Medical sciences
Pharmacology. Drug treatments
Rats
Rats, Wistar
Technetium Tc 99m Exametazime - chemical synthesis
Technetium Tc 99m Exametazime - chemistry
Technetium Tc 99m Exametazime - pharmacology
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Summary:Tc- d,d- and Tc- l,l-HMPAO were synthesized. The stability of Tc- d,d- and Tc- l,l-HMPAO in vitro is similar to that of d,l-isomers by the spectrophotometric and three strips methods. Cerebral uptake (%D in brain) for the l,l-isomer is higer than the d,d- and d,l-isomer in rats. Delayed studies shows that Tc- l,l-HMPAO reveals less washout and reflects a higher cerebral deposition properties than the d,d- and d,l-isomer. d,d- and 1,1-HMPAO were synthesized. Cerebral uptake (%D in brain) for the 1,1-isomer is higer than the d,d- and d,1-isomer in rats. Tc-1,1-HMPAO reveals less washout and reflects a higher cerebral deposition properties than the d,d- and d,1-isomer.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00557-0