Balasubramaniam S, Simons L A, Chang S
Atherosclerosis. 1986 Jun;60(3):263-8. doi: 10.1016/0021-9150(86)90173-5.
Ro 16-0521 is a newly synthesized benzodiazepine derivative which is devoid of reactivity with the brain benzodiazepine receptor. The effects of this drug on plasma lipids and lipoproteins and hepatic cholesterol metabolism have been examined in the cholesterol-fed rat. Drug therapy was associated with dose-related falls in plasma cholesterol concentration, liver cholesterol content, and the activity of the liver enzyme Acyl-CoA cholesterol acyltransferase. Drug therapy abolished the lipid and lipoprotein changes induced by cholesterol feeding, including those associated with a diet supplemented with olive oil to facilitate cholesterol loading. Drug therapy was also associated with an increased activity of the enzyme HMG-CoA reductase and reduced hepatic microsomal cholesterol content. It is suggested that the cholesterol-fed rat will be a suitable model for further mechanistic studies.
Ro 16-0521是一种新合成的苯二氮䓬衍生物，它与脑苯二氮䓬受体无反应性。已在喂食胆固醇的大鼠中研究了该药物对血浆脂质、脂蛋白和肝脏胆固醇代谢的影响。药物治疗与血浆胆固醇浓度、肝脏胆固醇含量以及肝脏酶酰基辅酶A胆固醇酰基转移酶活性的剂量相关下降有关。药物治疗消除了胆固醇喂养引起的脂质和脂蛋白变化，包括与添加橄榄油以促进胆固醇负荷的饮食相关的变化。药物治疗还与HMG-CoA还原酶活性增加和肝脏微粒体胆固醇含量降低有关。有人认为，喂食胆固醇的大鼠将是进一步进行机制研究的合适模型。
