SYNTHESIS OF METRONIDAZOLE DERIVATIVE AND ITS DiSTR!BUTION IN S_(180) BEARING MICE
- VernacularTitle:甲硝羟乙唑衍生物的合成和在荷S_(180)小鼠体内的分布
- Author:
Lixi YANG
- Publication Type:Journal Article
- Keywords:
metronidazole technetium sarcoma mice
- From:
Academic Journal of Second Military Medical University
1982;0(01):-
- CountryChina
- Language:Chinese
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Abstract:
A metronidazole derivative (CM) was synthesized by reaction of metronidazole on mitrilotriacetic acid.A series of analyses (eg.m.p.determination, TLC,paper ele-ctrophoresis & UV, IR)proved this synthetic compound to be metronidazole derivative. When labeled with99mTc, it produced 99mTc-CM, which could concentrate and maintain a high concentration in tumor in mice bearing sarcoma180 within 24 h after iv injection. The radioactiving ratio of 99mTc retained in tumor was about 10 and 5 as compared with that in muscle and brain, suggesting that 99mTc-CM has a strong tumor-localizing effect.Because of its lower concentration in the brain, its neuroto-xicity decreased. When CM was complexed with Ca+ + ,the product Ca-CM showed a strong ability to sensitize sarcoma180 to radiation(paper in preparation) .These results suggest that CM might be a new type of tumor-localizing and radiosensitizing compound. Further pharmacological experiments are in progress.
