N-ヘテロ芳香族の電子的性状(第60報)フェノチアジン系向精神薬の存在によるオキシヘモグロビンの酸化 : メトヘモグロビンの形成とその機構

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Studies were made on the oxidation of oxyhemoglobin (HbO_2) by the presence of phenothiazine system tranquilizers. Methemoglobin (MHb) was formed when a salt of ethopropazine (I), promethazine (II), promazine (III), or perazine (VI) was incubated with a suspension of human erythrocytes or with HbO_2 solution obtained through hemolysis of this suspension. In either of the experiments with erythrocytes and HbO_2 solution, the MHb-forming effect of the compound decreased in the order of I, II, III, and VI. The HbO_2-oxidizing activity of these derivatives was enhanced when they were photoirradiated before mixing of the derivatives with HbO_2 solution. Chlorpromazine, methoxypromazine, thioperazine, fluphenazine, trimeprazine, and methotrimeprazine formed MHb when their acid solutions were photoirradiated before their incubation with HbO_2 solution. The HbO_2-oxidizing activity of phenothiazine derivatives was also enhanced when they were subjected to potentiostatic electrolysis or pyrolysis. The amount of MHb formed in the incubation mixture paralleled the amount of semiquinone free radicals produced from the derivatives. On the basis of the results of comparative examinations on the HbO_2-oxidizing activity, spectral change in the ultraviolet and visible regions, and polarographic half-wave potentials of the derivatives, it was presumed that, in the case where untreated phenothiazine derivatives were involved, cation radicals produced by some oxidizing substance in the incubation mixture played an important role in the formation of MHb from HbO_2.
社団法人日本薬学会の論文
1977-04-25

N-ヘテロ芳香族の電子的性状(第60報)フェノチアジン系向精神薬の存在によるオキシヘモグロビンの酸化 : メトヘモグロビンの形成とその機構

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