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芬替酸的代谢

Metabolism of fentiazac.

作者信息

Fumero S, Mondino A, Silvestri S, Zanolo G, De Marchi G, Pedrazzini S

出版信息

Arzneimittelforschung. 1980;30(8):1253-6.

PMID:7192138
Abstract

The main metabolite of 2-phenyl-4-p-chlorophenylthiazol-5-ylacetic acid (fentiazac) is represented by a p-hydroxylated compound which is formed rapidly and that, still 72 later, can be detected in the general circulation. The p-hydroxylated metabolite is much less toxic than the original molecule from which it derives, being still active from an anti-inflammatory standpoint (its activity being equal to 70--75% of that of fentiazac). The metabolite, which possesses a therapeutic index much higher than that of fentiazac, represents quite an important step in the detoxication processes of the drug and enhances the therapeutic activity of the drug itself.

摘要

2-苯基-4-对氯苯基噻唑-5-基乙酸(芬替扎ac)的主要代谢产物是一种对羟基化化合物,它形成迅速,并且在72小时后仍可在全身循环中检测到。该对羟基化代谢产物的毒性远低于其衍生的原始分子,从抗炎角度来看仍具有活性(其活性相当于芬替扎ac的70%-75%)。该代谢产物的治疗指数远高于芬替扎ac,在药物解毒过程中是相当重要的一步,并增强了药物本身的治疗活性。

相似文献

1
Metabolism of fentiazac.芬替酸的代谢
Arzneimittelforschung. 1980;30(8):1253-6.
2
Pharmacokinetics of fentiazac in rats and monkeys.芬替酸在大鼠和猴子体内的药代动力学。
Arzneimittelforschung. 1981;31(7):1098-104.
3
Preliminary studies on the fate of 14C-fentiazac in man.14C-芬替酸在人体中的代谢初步研究。
Xenobiotica. 1984 Dec;14(12):956-60.
4
The pharmacokinetics of fentiazac and its metabolite, p-hydroxyfentiazac, after twice-daily oral administration to male volunteers.芬替酸及其代谢产物对羟基芬替酸在男性志愿者每日口服两次后的药代动力学。
Xenobiotica. 1984 Dec;14(12):947-53. doi: 10.3109/00498258409151493.
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A comparative study of the antiinflammatory activity of fentiazac and its major metabolite, p-hydroxy fentiazac.
Agents Actions. 1984 Oct;15(3-4):443-7. doi: 10.1007/BF01972385.
6
Metabolism of 2-(4-chlorophenyl)thiazol-4-ylacetic acid (fenclozic acid) and related compounds by microorganisms.微生物对2-(4-氯苯基)噻唑-4-乙酸(芬克洛酸)及相关化合物的代谢
J Med Chem. 1972 Oct;15(10):1040-5. doi: 10.1021/jm00280a012.
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[Studies on skin diffusion with biological membranes: topical preparations of fentiazac acid].[生物膜皮肤扩散研究:芬替酸的局部制剂]
Boll Chim Farm. 1984 Nov;123(11):512-20.
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The metabolism of C14-ICI 54,450 (myalex) in various species--an in vivo NIH shift.C14-ICI 54,450(麦亚历)在不同物种中的代谢——体内NIH转化。
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Metabolites and analogs of 2-ethyl-2,3-dihydro-5-benzofuranacetic acid (furofenac): chemical and pharmacological properties.2-乙基-2,3-二氢-5-苯并呋喃乙酸(呋罗芬酸)的代谢物及类似物:化学与药理学性质
J Pharm Sci. 1980 Feb;69(2):164-7. doi: 10.1002/jps.2600690212.
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[Relation between the anti-inflammatory activity and serum and tissue levels of rectally-administered fentiazac].[经直肠给药的芬替酸抗炎活性与血清及组织水平之间的关系]
Boll Chim Farm. 1982 Dec;121(12):632-47.

引用本文的文献

1
A comparative study of the antiinflammatory activity of fentiazac and its major metabolite, p-hydroxy fentiazac.
Agents Actions. 1984 Oct;15(3-4):443-7. doi: 10.1007/BF01972385.