[Cleavage and biotransformation of the central muscle relaxant chlormezanone].
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.
Institut für Pharmazie, Friedrich-Schiller-Universität, Jena, Germany.
H
H
Oelschläger
W
W
Klinger
D
D
Rothley
A
A
Seeling
H
H
Bockhard
B
B
Hofmann
H
H
Machts
H
H
Riederer
H
H
Rackur
D001711:Biotransformation; D002720:Chlormezanone / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D006207:Half-Life; D006801:Humans; D009125:Muscle Relaxants, Central / Q000493:pharmacokinetics*
D009125:Muscle Relaxants, Central; D002720:Chlormezanone
Spaltung und Biotransformation des zentralen Muskelrelaxans Chlormezanon.