The synthesis of 6'-hydroxycinchonine [8R,9S)-cinchonan-6',9-diol] was achieved by demethylating quinidine with boron tribromide in dichloromethane at -75 degrees C. The antiarrhythmic activities of 6'-hydroxycinchonine and quinidine were compared following the infusion of aconitine into the tail veins of mice to induce arrhythmias. Comparative ED50 and LD50 studies for quinidine and 6'-hydroxycinchonine revealed equivalent antiarrhythmic potencies for the two drugs but a smaller acute toxicity for 6'-hydroxycinchonine.
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Comparative pharmacokinetics of quinidine and its O-desmethyl metabolite in rabbits.
J Pharm Sci
December 1980
The pharmacokinetics of quinidine and the O-desmethyl metabolite 6'-hydroxycinchonine were studied in rabbits. After intravenous bolus injections of equimolar doses, the blood concentration-time curves of each agent declined biexponentially, which was characteristic of a two-compartment open model. A significant difference between quinidine and 6'-hydroxycinchonine was observed for the following parameters: t1/2 alpha, beta, t1/w beta, k12, Vd beta, and the intercompartmental distribution ratio, k12/k21.
View Article and Find Full Text PDFThe synthesis of 6'-hydroxycinchonine [8R,9S)-cinchonan-6',9-diol] was achieved by demethylating quinidine with boron tribromide in dichloromethane at -75 degrees C. The antiarrhythmic activities of 6'-hydroxycinchonine and quinidine were compared following the infusion of aconitine into the tail veins of mice to induce arrhythmias. Comparative ED50 and LD50 studies for quinidine and 6'-hydroxycinchonine revealed equivalent antiarrhythmic potencies for the two drugs but a smaller acute toxicity for 6'-hydroxycinchonine.
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