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氟他胺。一种新型非甾体抗雄激素的作用机制。

Flutamide. Mechanism of action of a new nonsteroidal antiandrogen.

作者信息

Sufrin G, Coffey D S

出版信息

Invest Urol. 1976 May;13(6):429-34.

PMID:1270239
Abstract

Flutamide is a new nonsteroidal antiandrogen useful in the treatment of prostatic carcinoma. The mechanism of action of this compound was investigated using the sex accessory tissue of the male rat. Flutamide was found to block the action of both endogenous and exogenous testosterone and, in addition, to be a potent inhibitor of testosterone-stimulated prostatic DNA synthesis. Moreover, it is capable of inhibiting prostatic nuclear uptake of androgen. Electron microscopic observations further confirm the antiandrogenic properties of flutamide.

摘要

氟他胺是一种新型非甾体类抗雄激素药物,可用于治疗前列腺癌。利用雄性大鼠的性附属组织对该化合物的作用机制进行了研究。发现氟他胺可阻断内源性和外源性睾酮的作用,此外,它还是睾酮刺激的前列腺DNA合成的强效抑制剂。而且,它能够抑制雄激素在前列腺细胞核内的摄取。电子显微镜观察进一步证实了氟他胺的抗雄激素特性。

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