title: Enantioselective metabolism of quizalofop-ethyl in rat.
abstract: The pharmacokinetic and distribution of the enantiomers of quizalofop-ethyl and its metabolite quizalofop-acid were studied in Sprague-Dawley male rats. The two pairs of enantiomers were determined using a validated chiral high-performance liquid chromatography method. Animals were administered quizalofop-ethyl at 10 mg kg(-1) orally and intravenously. It was found high concentration of quizalofop-acid in the blood and tissues by both intragastric and intravenous administration, and quizalofop-ethyl could not be detected through the whole study which indicated a quick metabolism of quizalofop-ethyl to quizalofop-acid in vivo. In almost all the samples, the concentrations of (+)-quizalofop-acid exceeded those of (-)-quizalofop-acid. Quizalofop-acid could still be detected in the samples even at 120 h except in brain due to the function of blood-brain barrier. Based on a rough calculation, about 8.77% and 2.16% of quizalofop-acid were excreted through urine and feces after intragastric administration. The oral bioavailability of (+)-quizalofop-acid and (-)-quizalofop-acid were 72.8% and 83.6%.
authors: Department of Applied Chemistry, China Agricultural University, Beijing, PR China.
authors: Yiran
authors: Y
authors: Liang
authors: Department of Applied Chemistry, China Agricultural University, Beijing, PR China.
authors: Peng
authors: P
authors: Wang
authors: Department of Applied Chemistry, China Agricultural University, Beijing, PR China.
authors: Donghui
authors: D
authors: Liu
authors: Department of Applied Chemistry, China Agricultural University, Beijing, PR China.
authors: Zhigang
authors: Z
authors: Shen
authors: Department of Applied Chemistry, China Agricultural University, Beijing, PR China.
authors: Hui
authors: H
authors: Liu
authors: Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, PR China.
authors: Zhixin
authors: Z
authors: Jia
authors: Department of Applied Chemistry, China Agricultural University, Beijing, PR China.
authors: Zhiqiang
authors: Z
authors: Zhou
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D008297:Male; D011422:Propionates / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D011810:Quinoxalines / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013237:Stereoisomerism; D013379:Substrate Specificity; D014018:Tissue Distribution
chemical_list: D011422:Propionates; D011810:Quinoxalines; C477202:quizalofop; C064835:quizalofop-ethyl