In vitro diazepam metabolism in horses.

IF 0.4 4区 农林科学 Q4 VETERINARY SCIENCES Japanese Journal of Veterinary Research Pub Date : 2013-02-01
Aki Hayami, Wageh Sobhy Darwish, Yoshinori Ikenaka, Shouta M M Nakayama, Mayumi Ishizuka
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Abstract

There is little information about drug metabolism and pharmacokinetics in horses. Therefore, it is necessary to characterize the profiles of drug metabolites for the safe use of drugs. In this study, we focused on cytochrome P450 enzymes (CYPs), which represent an important enzyme group to determine pharmacological effects of drugs. We chose diazepam as the drug of choice for this study. The aim of this study was to elucidate the metabolic pathway of diazepam in horses in comparison with rats, and to clarify CYP subfamilies responsible for diazepam metabolism in horses. Our results showed temazepam was the major diazepam metabolite produced from microsomal reactions in horse liver, but horses produced drastically less p-hydroxydiazepam as compared with rats. Furthermore, CYP3A was a major contributor from the CYP subfamily of temazepam production.

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地西泮在马体内的体外代谢。
关于马的药物代谢和药代动力学的信息很少。因此,有必要对药物代谢产物的特征进行表征,以确保药物的安全使用。在本研究中,我们重点研究了细胞色素P450酶(CYPs),它是决定药物药理作用的重要酶群。我们选择地西泮作为本研究的首选药物。本研究的目的是通过与大鼠的比较,阐明地西泮在马体内的代谢途径,并阐明与马体内地西泮代谢有关的CYP亚家族。我们的研究结果表明,替马西泮是马肝脏微粒体反应产生的地西泮的主要代谢物,但与大鼠相比,马产生的对羟基地西泮明显减少。此外,CYP3A是替马西泮产生的CYP亚家族的主要贡献者。
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来源期刊
CiteScore
1.00
自引率
0.00%
发文量
0
审稿时长
>36 weeks
期刊介绍: The Japanese Journal of Veterinary Research (JJVR) quarterly publishes peer-reviewed articles on all aspects of veterinary science. JJVR was originally published as a “University Journal” of veterinary science at Hokkaido University from more than 60 years ago. Currently, JJVR, is Japan’s leading scientific veterinary journal, and provides valuable information for the development of veterinary science by welcoming contributions from researchers worldwide. JJVR offers online submission for Regular Papers, Short Communications, and Review Articles that are unpublished and not being considered for publication elsewhere. Research areas include: Anatomy, Physiology, Biochemistry, Pharmacology, Microbiology, Infectious diseases, Parasitology, Laboratory Animal Science and Medicine, Internal Medicine, Surgery, Pathology, Theriogenology, Molecular Medicine, Public Health, Radiation Biology, Toxicology, Wildlife Biology and Medicine, Veterinary Hygiene, The other fields related to veterinary science.
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