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[中枢性肌肉松弛剂氯美扎酮的裂解与生物转化]

[Cleavage and biotransformation of the central muscle relaxant chlormezanone].

作者信息

Oelschläger H, Klinger W, Rothley D, Seeling A, Bockhard H, Hofmann B, Machts H, Riederer H, Rackur H

机构信息

Institut für Pharmazie, Friedrich-Schiller-Universität, Jena, Germany.

出版信息

Pharmazie. 1998 Sep;53(9):620-4.

PMID:9770210
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.

摘要

氯美扎酮是一种手性中枢性肌肉松弛剂,它会通过自质子转移过程在其S-C-1键处发生裂解。在pH 2至pH 9之间存在化学稳定性的最佳范围,在pH 7.4时达到最大值。37℃时的血浆半衰期为76小时。酶确实会攻击裂解产物,即4-氯苯甲醛和2-羧基乙烷-亚磺酸-N-甲基酰胺。尿液中的主要代谢产物是4-氯马尿酸,其含量高达给予人类口服剂量的70%。细胞色素P-450不参与S-C键的裂解。

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