チオペンタール ^<35>S : 合成, 同位体希釈分析およびラットにおける代謝

概要

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Thiopental-^<35>S having a specific radioactivity of 13.2 mCi/mmole was synthesized from H_2^<35>SO_4 as the starting material through H_2^<35>S and thiourea-^<35>S. Radiochemical and chemical yields from H_2^<35>SO_4 were 80.3 and 85.7%, respectively. The isotope dilution analysis for the determination of commercial thiopental sodium preparations was investigated with the ^<35>S-labeled thiopental, and it gave the mean recovery of 99.60±0.68%. This method was advantageous over other known official methods such as ultraviolet absorptiometry and gravimetric analysis in the precision and selectivity of the method. As the metabolites of thiopental in the liver of male rats, methionine, thiourea, inorganic sulfate, and several unidentified ^<35>S-containing compounds were recognized by radiopaperscannography or reverse isotope dilution method. Metabolic rates of thiopental-^<35>S in rat liver were 0,49.7,59.2,and 60.2% at 15,30,90,and 120 minutes after its intraperitoneal injection, respectively. It was proved that a considerable amount of radioactivities arising from the injected ^<35>S-labeled thiopental was distributed in rat brain within 15 minutes after its intraperitoneal adminstration, and that the rapid reduction in radioactivities was found to three-fifths of the original during the following 15 minutes.
公益社団法人日本薬学会の論文
1969-09-25