EFFECT OF S-TRIAZINE COMPOUNDS ON TESTOSTERONE-METABOLISM IN THE RAT PROSTATE
EFFECT OF S-TRIAZINE COMPOUNDS ON TESTOSTERONE-METABOLISM IN THE RAT PROSTATE
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DOI：
10.1002/jat.2550150312
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发表时间：
1995-05-01
影响因子：
3.3
通讯作者：
KNIEWALD, Z
中科院分区：
文献类型：
--
作者：
KNIEWALD, J;OSREDECKI, V;KNIEWALD, Z
在大鼠前列腺中，研究了s-三嗪化合物（莠去津、扑草净和去乙基莠去津）对睾酮转化和5 α-二氢睾酮-受体复合物形成的影响。莠去津和扑草净（0.465 - 1.392 μ mol）及其混合物（总浓度为0.928 μ mol）对5 α-二氢睾酮的形成有明显的影响。0.5μ mol阿特拉津或脱乙基阿特拉津，仅在体内通过6 mg阿特拉津100 g（-1）体重。在前列腺胞质溶胶中，每天一次，持续7天。负责睾酮转化和类固醇激素受体复合物形成的酶活性的抑制是非竞争性和可逆的，和s-三嗪化合物作为抗雄激素。
The influence of s-triazine compounds (atrazine, prometryne and deethylatrazine) on testosterone conversion and 5 alpha-dihydrotestosterone-receptor complex formation was studied in vitro and in vivo in the rat prostate. A marked in vitro influence of atrazine and prometryne (from 0.465 to 1.392 mu mol) and their mixtures (in total concentration, 0.928 mu mol) on 5 alpha-dihydrotestosterone formation was detected, 5 alpha-Dihydrotestosterone-specific receptor complex formation was inhibited in vitro by ca. 0.5 mu mol of atrazine or deethylatrazine and only in vivo by 6 mg of atrazine 100 g(-1) body wt. daily during 7 days in the prostate cytosol. The inhibition of the enzymic activities responsible for testosterone conversion and steroid hormone-receptor complex formation was non-competitive and reversible, and s-triazine compounds act as antiandrogens.