CLEAVAGE ACID BIOTRANSFORMATION OF THE CENTRALLY ACTING MUSCLE-RELAXANT CHLORMEZANONE

Citation
H. Oelschlager et al., CLEAVAGE ACID BIOTRANSFORMATION OF THE CENTRALLY ACTING MUSCLE-RELAXANT CHLORMEZANONE, Die Pharmazie, 53(9), 1998, pp. 620-624
Citations number
10
Categorie Soggetti
Pharmacology & Pharmacy","Chemistry Medicinal",Chemistry
Journal title
ISSN journal
00317144
Volume
53
Issue
9
Year of publication
1998
Pages
620 - 624
Database
ISI
SICI code
0031-7144(1998)53:9<620:CABOTC>2.0.ZU;2-R
Abstract
Chlormezanone, a chiral centrally acting muscle relaxant, will be clea ved at its S-C-1 bond by an autoprotolytic process. The optimum of che mical 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-chloroh ippuric acid in the range of up to 70% of the oral administered dose t o humans. No cytochrome P-450 is engaged in the cleavage of the S-C-bo nd.