亚油酰胺的代谢。I. N-（α-甲基苄基）亚油酰胺在大鼠和人体中的吸收、排泄及代谢

Metabolism of linoleamides. I. Absorption, excretion and metabolism of N-(alpha-methylbenzyl)linoleamide in rat and man.

Hirohashi A, Nagata A, Miyawaki H, Nakatani H, Toki K

Xenobiotica. 1976 Jun;6(6):329-37. doi: 10.3109/00498257609151644.

Abstract

In urine of rats dosed with N-(alpha-methylbenzyl)linoleamide (MBLA), three dicarboxylic acid monoamides, N-(alpha-methylbenzyl)succinic acid monoamide, N-(alpha-methylbenzyl)glutaric acid monoamide and N-(alpha-methylbenzyl)adipic acid monoamide, were identified. Conjugated alpha-methylbenzylamine, hippuric acid and conjugates of the dicarboxylic acid monoamides were also found in the urine. N-(alpha-Methylbenzyl)succinic acid monoamide was the main metabolite in rats. 2. Biliary excretion of radioactivity was studied in rats, cannulated for collection of bile and duodenal infusion, after oral administration of N-(alpha-methylbenzyl)[1-14C]linoleamide. With constant duodenal infusion of bile, about 7% of the dose was excreted in the bile, while excretion of radioactivity was negligible without bile infusion. 3. The g.l.c. analysis of human urine after oral administration of MBLA revealed that two dicarboxylic acid monoamides were present and N-(alpha-methylbenzyl)succinic acid monoamide was the main metabolite. 4. MBLA was excreted unchanged in the faeces of men who received MBLA to the extent of about 53% dose in 3 days. 5. MBLA was not detected (less than 1 mug/ml) in the serum of a volunteer who had been taking an oral daily dose of 1500 mg of MBLA for 3 months.

摘要

在给予N-（α-甲基苄基）亚油酰胺（MBLA）的大鼠尿液中，鉴定出三种二羧酸单酰胺，即N-（α-甲基苄基）琥珀酸单酰胺、N-（α-甲基苄基）戊二酸单酰胺和N-（α-甲基苄基）己二酸单酰胺。尿液中还发现了结合型α-甲基苄胺、马尿酸以及二羧酸单酰胺的结合物。N-（α-甲基苄基）琥珀酸单酰胺是大鼠体内的主要代谢产物。2. 对经胆管插管以收集胆汁并进行十二指肠灌注的大鼠，口服给予N-（α-甲基苄基）[1-¹⁴C]亚油酰胺后，研究其放射性胆汁排泄情况。在十二指肠持续灌注胆汁的情况下，约7%的给药剂量经胆汁排泄，而在无胆汁灌注时，放射性排泄可忽略不计。3. 口服MBLA后对人尿液进行气相色谱分析表明，存在两种二羧酸单酰胺，且N-（α-甲基苄基）琥珀酸单酰胺是主要代谢产物。4. 接受MBLA的男性粪便中MBLA未发生变化，在3天内排泄量约为给药剂量的53%。5. 一名志愿者每日口服1500 mg MBLA，持续3个月，其血清中未检测到MBLA（低于1 μg/ml）。