Marquie G
Atherosclerosis. 1979 Mar;32(3):253-7. doi: 10.1016/0021-9150(79)90168-0.
The effects of the novel fenfluramine derivative, S 1204 (meta-trifluoromethyl phenyl-1 [beta(sulfamyl-3'-chloro-4'-benzoyloxyethyl)]amino-2-propane) were studied on lipid metabolism in rabbit aorta and other tissues. Pretreatment of rabbits with S 1204 (50 mg/kg orally) for 10 days strongly inhibited the aortic incorporation of an intravenous 20 muCi tracer-dose of [4-(14)C]-cholesterol given 24 h earlier. However, incorporation of such cholesterol radioactivity into the liver, intestine, lung or plasma was not affected, in comparison with control animals. One hour after i.v. injection of a 100 muCi tracer-dose of [2-(14)C]acetate, S 1204 significantly reduced the radioactivity of total lipids in the aorta and liver. Such inhibition of acetate incorporation into arterial lipids was observed with all lipid fractions (that is, free fatty acids, esterified cholesterol, especially phospholipids, glycerides and free cholesterol). Incorporation of acetate into intestinal triglyceride fractions was also significantly decreased. The results indicate that S 1204 may have anti-atherogenic properties, which could be valuable in the clinical treatment of atherosclerosis.
研究了新型芬氟拉明衍生物S 1204（间三氟甲基苯基-1-[β-(氨磺酰基-3'-氯-4'-苯甲酰氧基乙基)]氨基-2-丙烷）对兔主动脉及其他组织脂质代谢的影响。用S 1204（50毫克/千克口服）预处理兔子10天，可强烈抑制24小时前静脉注射的20微居里示踪剂量[4-(14)C]-胆固醇在主动脉中的掺入。然而，与对照动物相比，这种胆固醇放射性掺入肝脏、肠道、肺或血浆中的情况未受影响。静脉注射100微居里示踪剂量的[2-(14)C]乙酸盐1小时后，S 1204显著降低了主动脉和肝脏中总脂质的放射性。在所有脂质组分（即游离脂肪酸、酯化胆固醇，尤其是磷脂、甘油酯和游离胆固醇）中均观察到乙酸盐掺入动脉脂质的这种抑制作用。乙酸盐掺入肠道甘油三酯组分的情况也显著减少。结果表明，S 1204可能具有抗动脉粥样硬化特性，这在动脉粥样硬化的临床治疗中可能具有重要价值。
