Aki Hayami, Wageh Sobhy Darwish, Yoshinori Ikenaka, Shouta M M Nakayama, Mayumi Ishizuka
{"title":"地西泮在马体内的体外代谢。","authors":"Aki Hayami, Wageh Sobhy Darwish, Yoshinori Ikenaka, Shouta M M Nakayama, Mayumi Ishizuka","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":56285,"journal":{"name":"Japanese Journal of Veterinary Research","volume":null,"pages":null},"PeriodicalIF":0.4000,"publicationDate":"2013-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"In vitro diazepam metabolism in horses.\",\"authors\":\"Aki Hayami, Wageh Sobhy Darwish, Yoshinori Ikenaka, Shouta M M Nakayama, Mayumi Ishizuka\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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.</p>\",\"PeriodicalId\":56285,\"journal\":{\"name\":\"Japanese Journal of Veterinary Research\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.4000,\"publicationDate\":\"2013-02-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Japanese Journal of Veterinary Research\",\"FirstCategoryId\":\"97\",\"ListUrlMain\":\"\",\"RegionNum\":4,\"RegionCategory\":\"农林科学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"VETERINARY SCIENCES\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Japanese Journal of Veterinary Research","FirstCategoryId":"97","ListUrlMain":"","RegionNum":4,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"VETERINARY SCIENCES","Score":null,"Total":0}
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.
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.
分享
京公网安备 11010802042870号
京ICP备2023020795号-1
求助内容：
应助结果提醒方式：
扫码关注我们
