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A Critique on the Evaluation and Mode of Action of Antiestrogens

 

作者: M.S. Sankaran,   M.R.N. Prasad,  

 

期刊: Gynecologic and Obstetric Investigation  (Karger Available online 1972)
卷期: Volume 3, issue 1-4  

页码: 142-147

 

ISSN:0378-7346

 

年代: 1972

 

DOI:10.1159/000301751

 

出版商: S. Karger AG

 

关键词: Estrogen action at the estrogen sensitive target organs

 

数据来源: Karger

 

摘要:

(1) The ‘true antiestrogens’ are estrogenic and are competitive inhibitors of estrogen action at the estrogen-sensitive target organs. The estrogenicity of a compound needs to be specified with reference to (a) the target tissue, (b) parameter used, (c) route of administration, (d) dose of the compound, (e) time sequence of action. The degree of antiestrogenicity is directly proportional to the, estrogenicity of the compound. The antiestrogenic action of a compound is related to its affinity with the receptor sites in the target organ: (a) compounds which are bound to the receptors for brief periods are weakly estrogenic (DMS, cis-clomiphene), (b) compounds which have greater binding affinity with the receptors in the target organ are strongly estrogenic and antiestrogenic (CN 55, 945–27; trans-clomiphene, DES, MER-25 at high doses). The duration of antiestrogenic action of a compound is related to the duration of its binding with the receptor in the target organ.

 

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