Keio University · 의학
히사카즈 오타니 교수의 연구실은 약물 대사 및 약물 상호작용, 특히 시토퍼린 P450 효소, 특히 CYP3A4 유전자 변형이 약물 대사에 미치는 영향을 중심으로 연구를 진행하고 있습니다. 심장 부정맥 유발 가능성, 식이 콜레스테롤과 지방산의 대사적 영향, 그리고 항생제의 심전도 변화 등 약리학적·생화학적 기전을 정량적으로 분석하는 데 초점을 맞추고 있습니다. 특히 메커니즘 기반 억제(MBI)와 경쟁적 억제의 차이를 CYP3A4 유전자 아형에 따라 규명하는 데 기여하고 있습니다.
표시된 성과는 수집된 데이터 기준으로 산출되며, 일부 차이가 있을 수 있습니다.
The effects of dietary cholesterol and fatty acids on the plasma cholesterol level and rates of very low density lipoprotein (VLDL) cholesterol secretion and low density lipoprotein (LDL) transport through LDL receptors in the liver of the hamster were investigated. Increases of plasma VLDL- and LDL-cholesterol levels and VLDL-cholesterol secretion from hepatocytes were observed in animals fed a diet enriched with 0.1% cholesterol for 2 weeks in comparison with animals fed a control diet. The ad
In order to evaluate the arrhythmogenic potency of macrolide antibiotics in a quantitative manner, we analyzed the influence of clarithromycin (CAM), roxithromycin (RXM), and azithromycin (AZM) on Q-T intervals from pharmacokinetic and pharmacodynamic points of view and in comparison with the potency of erythromycin (EM) previously reported by us for rats. Male Sprague-Dawley rats were anesthetized, and CAM (6.6, 21.6, and 43.2 mg/kg of body weight/h), RXM (20 and 40 mg/kg/h), and AZM (40 and 10
Inhibition of cytochrome P450 (CYP) 3A4 is the major cause of drug-drug interactions (DDI). We have previously reported that the genetic variation of CYP3A4 significantly affected the inhibitory profiles of typical competitive inhibitors. In addition to competitive inhibition, some clinically significant DDI are attributable to mechanism-based inhibition (MBI). However, the differences in the MBI kinetics among CYP3A4 genetic variants remain to be characterized. In this study, we quantitatively