anabolic-androgenic类固醇的相对亲和力:比较绑定在骨骼肌雄激素受体在前列腺癌,以及性hormone-binding球蛋白。
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Saartok T, Dahlberg E, Gustafsson农协
anabolic-androgenic类固醇的相对亲和力:比较绑定在骨骼肌雄激素受体在前列腺癌,以及性hormone-binding球蛋白。
内分泌学。1984年6月,114 (6):2100 - 6。doi: 10.1210 / endo - 114 - 6 - 2100。
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6539197 (在PubMed]
- 文摘
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目前尚不清楚合成代谢类固醇作用于骨骼肌通过雄激素受体(AR)在这个组织,或是否有单独的合成受体。当几个合成代谢类固醇测试作为竞争对手的绑定[3 h] methyltrienolone(太;17 beta-hydroxy-17 alpha-methyl-4 9 11-estratrien-3-one) AR在鼠和兔骨骼肌和大鼠前列腺,分别太本身是最有效的竞争对手。1 alpha-Methyl-5 alpha-dihydrotestosterone (1 alpha-methyl-DHT;美睾酮)绑定热衷于性hormone-binding球蛋白(SHBG)相对亲和力(RBA) (DHT)的4倍。beplayapp一些anabolic-androgenic类固醇强烈约束的基于“增大化现实”技术的骨骼肌和前列腺(澳大利亚央行相对的MT:太大于19-nortestosterone (NorT;诺龙)大于methenolone (17 beta-hydroxy-1-methyl-5 alpha-androst-1-en-3-one)大于睾酮(T)大于1 alpha-methyl-DHT]。在其他情况下,基于“增大化现实”技术的结合很弱(RBA值小于0.05):康力龙(17 alpha-methyl-5α- androstano [3、2 c] pyrazol-17 beta-ol), methanedienone (17 beta-hydroxy-17 alpha-methyl-1, 4-androstadien-3-one),和fluoxymesterolone (9 alpha-fluoro-11 beta-hydroxy-17 alpha-methyl-T)。其他化合物rba太低待定(例如oxymetholone (17 beta-hydroxy-2-hydroxymethylene-17 alpha-methyl-5 alpha-androstan-3-one)和ethylestrenol (17 alpha-ethyl-4 - estren -17 beta-ol)。竞争模式类似于肌肉和前列腺,除了更高的澳大利亚央行DHT的前列腺。 The low RBA of DHT in muscle was probably due to the previously reported rapid reduction of its 3-keto function to metabolites, which did not bind to the AR [5 alpha-androstane-3 alpha, 17 beta-diol and its 3 beta-isomer (3 alpha- and 3 beta-adiol, respectively)]. Some anabolic-androgenic steroids (only a few synthetic) bound to SHBG (1 alpha-methyl-DHT much greater than DHT greater than T greater than 3 beta-adiol greater than 3 alpha-adiol = 17 alpha-methyl-T greater than methenolone greater than methanedienone greater than stanozolol). The ratio of the RBA in rat muscle to that in the prostate (an estimate of the myotrophic potency of the compounds) was close to unity, varying only between about 0.4 and 1.7 in most cases.(ABSTRACT TRUNCATED AT 400 WORDS)