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新型降血脂药2-(4-氯苯基)-5-(2-呋喃基)-恶唑-4-乙酸乙酯在大鼠、兔和犬体内的代谢。羧基的葡萄糖醛酸化及呋喃环的裂解。

Metabolism of ethyl 2-(4-chlorophenyl)-5-(2-furyl)-oxazole-4-acetate, a new hypolipidemic agent, in the rat, rabbit, and dog. Glucuronidation of carboxyl group and cleavage of furan ring.

作者信息

Kobayashi T, Ando H, Sugihara J, Harigaya S

出版信息

Drug Metab Dispos. 1987 Mar-Apr;15(2):262-6.

PMID:2882988
Abstract

Metabolism of ethyl 2-(4-chlorophenyl)-5-(2-furyl)-oxazole-4-acetate (TA-1801), a new hypolipidemic agent, was studied in the rat, rabbit, and dog. Animals were given a single oral dose of 50 mg/kg TA-1801 labeled with 14C. The first metabolic reaction for TA-1801 was hydrolysis of the ester linkage. The resulting metabolite M1 was found to undergo further biotransformations, i.e. glucuronidation at the carboxyl group and ring cleavage of the furan group. These metabolic pathways were observed in all the species examined, although species differences were seen in the amount of metabolites.

摘要

新型降血脂药物2-(4-氯苯基)-5-(2-呋喃基)恶唑-4-乙酸乙酯(TA-1801)在大鼠、兔子和狗体内的代谢情况进行了研究。给动物单次口服50mg/kg用14C标记的TA-1801。TA-1801的首个代谢反应是酯键水解。发现生成的代谢物M1会进一步发生生物转化,即羧基的葡萄糖醛酸化和呋喃基团的环裂解。在所有受试物种中均观察到了这些代谢途径,不过在代谢物的量上存在物种差异。

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