[Study on the metabolites of cui-xing-an in rat urine].
m-[(2-Dimethylamino) ethoxy] phenyl-N, N-dimethyl carbamate (Cui-Xing-An) is a new central anticholinesterase drug. After oral administration of Cui-Xing-An to rats, four components were isolated and purified from urine extract by HPLC. They were identified by MS to be the parent drug, m-[2-dimethylamino) ethoxy] phenyl-N-hydroxymethyl-N-methyl carbamate (hydroxylated Cui-Xing-An), m-[(2-dimethylamino) ethoxy] phenyl-N-methyl carbamate (N-demethylated Cui-Xing-An) and m-[(2-dimethylamino) ethoxy] phenol (hydrolysate). Experiment on Torpediniforms Nacline timilei AchE inhibitory rate showed that the N-demethyl Cui-Xing-An had the same anticholinesterase activity as the parent drug. The hydroxylated Cui-Xing-An exhibited lower activity, and the hydrolysate was inactive.
Li
H
H
Ruan
J X
JX
Tang
B S
BS
Wu
L M
LM
Jia
J S
JS
D000470:Alkaloids / Q000493:pharmacokinetics* / Q000652:urine; D000818:Animals; D002800:Cholinesterase Inhibitors / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D008658:Inactivation, Metabolic; D008297:Male; D013058:Mass Spectrometry; D051381:Rats
D000470:Alkaloids; D002800:Cholinesterase Inhibitors; C034764:cui xing an