Pharmacokinetic and tumour-penetration properties of the hypoxic cell radiosensitizer desmethylmisonidazole (Ro 05-9963) in dogs

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Summary: International Symposium on the Health Effects of Boron and its Compounds.

-The hypoxic cell radiosensitizer desmethylmisonidazole (1-(2-nitroimidazol-1-yl)-2,3-propandiol; Ro 05-9963; DEMIS) was administered to 4 dogs at doses of 50 and 200 mg/kg by both oral and i.v. routes. The resulting plasma, cerebro spinal fluid and urinary concentrations were measured by HPLC analysis; various pharmacokinetic parameters were obtained and compared with similar data for the pare...

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-Concentrations of the hypoxic cell radiosensitizer misonidazole (MIS) and its 0 -demethylated metabolite Ro 05 -9963 were determined in plasma (or blood), brain and tumour after injection of I g/kg MIS i.p. to control mice or mice pretreated with 4-6 daily injections of phenobarbitone or phenytoin. Analysis was by highperformance liquid chromatography (HPLC). Phenobarbitone and phenytoin did n...

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-Bilateral kidney ligation of mice immediately before injection of misonidazole (MIS) prolongs the plasma half-life of this radiosensitizer from about 2 h (in normal mice) to 10-11 h, similar to that in man. Kidney ligation does not, however, change the relative proportions of MIS and its 0-demethylated metabolite, Ro-05-9963, for the first 12 h after MIS injection. Kidney ligation was used wit...

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ژورنال

عنوان ژورنال: British Journal of Cancer

سال: 1980

ISSN: 0007-0920,1532-1827

DOI: 10.1038/bjc.1980.39