Abstract
The metabolism of methylscopolammonium methylsulfate (I) in rats was investigated. Eight metabolites were detected in urine and faeces after oral and subcutaneous administrations. The feature of metabolic pathway was characterized as follows ; i) the quarternary ammonium moiety was unchanged, ii) major pathway involved oxidation at the paraposition of benzene ring to introduce a hydroxy and a methoxy groups, iii) minor products were the apo-derivative, glucuronide of I and scopine derivative. Absorption and excretion were examined by using 14C-labeled compound, and excreted total radioactivities were 82.2% of oral dose and 93.6% of subcutaneous dose in urine and faeces. In respiratory air 14CO2 was not detectable. Comparison of the metabolic pathway with that of tertiary scopolamine are also discussed.
