1. [Cleavage and biotransformation of the central muscle relaxant chlormezanone].
- Author
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Oelschläger H, Klinger W, Rothley D, Seeling A, Bockhard H, Hofmann B, Machts H, Riederer H, and Rackur H
- Subjects
- Biotransformation, Chromatography, High Pressure Liquid, Half-Life, Humans, Chlormezanone pharmacokinetics, Muscle Relaxants, Central pharmacokinetics
- Abstract
Chlormezanone, a chiral centrally acting muscle relaxant, will be cleaved at its S-C-1 bond by an autoprotolytic process. The optimum of chemical stability exists between pH 2 up to pH 9 with a maximum at pH 7.4. The plasma half life at 37 degrees C is 76 h. Enzymes do attack the products of cleavage namely 4-chlorobenzaldehyde and 2-carboxyethane-sulfinic-acid-N-methyl-amide. The main metabolite in urine is 4-chlorohippuric acid in the range of up to 70% of the oral administered dose to humans. No cytochrome P-450 is engaged in the cleavage of the S-C-bond.
- Published
- 1998