Stereoselective toxicokinetics and tissue distribution of ethofumesate in rabbits.
The stereoselective toxicokinetics of ethofumesate enantiomers following a single intravenous (i.v.) administration at doses of 30 mg/kg were investigated in rabbits. Plasma concentrations of (+)- and (-)-ethofumesate were analyzed by a validated chiral HPLC method that involved extraction of plasma with organic solvent followed by separation on a cellulose-Tris-(3,5-dimethylphenylcarbamate)-based chiral column and quantification by UV absorbance at 230 nm. Plasma concentration-time curves after i.v. administration were best described by an open two-compartment model. The concentration of the (-)-enantiomer decreased more rapidly than that of the (+)-enantiomer. Significant differences in toxicokinetic parameters between the two enantiomers indicated that stereoselective behavior occurred with the (-)-enantiomer being preferentially metabolized and eliminated.
Zhu
Wentao
W
Department of Applied Chemistry, China Agricultural University, Beijing, People's Republic of China.
Dang
Ziheng
Z
Qiu
Jing
J
Lv
Chunguang
C
Jia
Guifang
G
Li
Li
L
Zhou
Zhiqiang
Z
D000818:Animals; D001572:Benzofurans / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics* / Q000633:toxicity*; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D006540:Herbicides / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D008297:Male; D008698:Mesylates / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics* / Q000633:toxicity*; D011817:Rabbits; D013237:Stereoisomerism; D014018:Tissue Distribution
D001572:Benzofurans; D006540:Herbicides; D008698:Mesylates; C412911:ethofumesate