title: The enantioselective pharmacokinetics metabolism of diniconazole in quail (Coturnix coturnixs japonica).
abstract: The pharmacokinetics of diniconazole enantiomers in quail (Coturnix coturnix japonica) were investigated by liquid chromatography-tandem mass spectrometry (LC-MS/MS). Quails were exposed to racemic diniconazole in capsule by oral at dose of 10 mg/kg (body weight). The maximal concentrations observed in blood, heart, liver, and kidney were 3.18, 11.35, 12.32, 15.03 µg/g for S-diniconazole, and 1.13, 3.70, 6.00, 2.60 µg/g for R-diniconazole. The elimination of enantiomers all met the one-compartment model in blood, heart, liver, and kidney well. The elimination half-lives (T1/2) of S-diniconazole were 2.87, 3.85, 5.29, and 4.42 h in blood, heart, liver, and kidney, respectively; the T1/2 of R-diniconazole were 2.44, 3.42, 146.23, and 74.02 h in blood, heart, liver, and kidney, respectively. The enantiomer fractions (EFs) steadily increased from 0.50 to 0.92 in blood samples and 0.91 in heart samples. Meanwhile, the values increased to 0.70 and 0.80 in liver and kidney initially, and then decreased to 0.33 and 0.44 at the end of the experiment. Metabolism was examined as well and it was found that diniconazole was metabolized to 1, 2, 4-triazole, (E)-3-(1H-1, 2, 4-triazol-1-yl) acrylaldehyde, (E, S)-(R, S)-4-(2, 4-dichlorophenyl)-2, 2-dimethyl-5-(1H-1, 2, 4-triazol-1-yl) pent-4-ene-1, 3-diol, (E)-4-(2, 4-dichlorophenyl)-3-hydroxy-2, 2-dimethyl-5-(1H-1, 2, 4-triazol-1-yl) pent-4-enoic acid, and 1, 3-dichlorobenzen in all samples of quail.
authors.affiliation: Research Center for Eco-Environmental Sciences, Chinese Academy of Sciences, Beijing, P.R. China.
authors.forename: Jin Hui
authors.initials: JH
authors.lastname: Chen
authors.forename: Hui Li
authors.initials: HL
authors.lastname: Wang
authors.forename: Bao Yuan
authors.initials: BY
authors.lastname: Guo
authors.forename: Peng
authors.initials: P
authors.lastname: Xu
authors.forename: Jian Zhong
authors.initials: JZ
authors.lastname: Li
mesh_terms: D000818:Animals; D007668:Kidney / Q000378:metabolism; D008099:Liver / Q000378:metabolism; D015394:Molecular Structure; D009206:Myocardium / Q000378:metabolism; D011784:Quail; D013237:Stereoisomerism; D053719:Tandem Mass Spectrometry; D014230:Triazoles / Q000097:blood / Q000378:metabolism / Q000493:pharmacokinetics*
chemical_list: D014230:Triazoles; C049346:diniconazole
keywords: diniconazole; enantioselectivity; metabolism; pharmacokinetics; quail