抑制雌激素及抗雌激素的uterotropic活动短效抗雌激素LY117018。

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约旦VC, Gosden B

抑制雌激素及抗雌激素的uterotropic活动短效抗雌激素LY117018。

内分泌学。1983年8月,113 (2):463 - 8。

PubMed ID

6872937 (在PubMed

]

文摘

这项研究的目的是确定二羟抗雌激素LY117018,与雌激素受体的高亲和力、低内在雌激素活性,能够抑制uterotropic甾族的行为[estradiol-17β(E2)]和非甾体类(ICI 3188和trianisylchloroethylene (TACE)雌激素在不成熟的老鼠和它莫西芬的uterotropic行为和monohydroxytamoxifen切除卵巢的老鼠和不成熟的老鼠。第一系列的实验LY117018 monohydroxytamoxifen相比。两种抗雌激素抑制E2的uterotropic行为(0.32毫克每天),这里3188(5毫克每天),别说话(40和160毫克每日)在剂量(0.32 -82毫克每天)。抗雌激素的力量对E2和ICI 3188相似,然而,在高剂量(20.48和82毫克每天)LY117018子宫重量减少到低于通过monohydroxytamoxifen的最低水平。相比之下,LY117018长少有效对抗雌激素别说话。的竞争互动LY117018与他莫昔芬和monohydroxytamoxifen在为期3天的切除卵巢的老鼠相比,未成熟大鼠子宫重量测试。他莫昔芬和monohydroxytamoxifen完全雌激素在鼠标(5毫克每天)和部分雌激素在鼠(1.5 -20毫克每天)。LY117018部分雌激素在鼠标和每周活跃的局部雌激素鼠(2.5 -120毫克每天)。LY117018产生剂量减少子宫重量增加引起的他莫昔芬和monohydroxytamoxifen物种。然而,在老鼠,LY117018更有效对抗引起的复合它莫西芬,在6:1剂量率而24:1的复合monohydroxytamoxifen所需剂量率。 LY117018 had a short duration of action as an antiestrogen when compared with monohydroxytamoxifen. LY117018 (120 micrograms) was only completely effective as an antiestrogen if administered repeatedly with E2 whereas a single injection of monohydroxytamoxifen (120 micrograms) was sufficient to inhibit fully E2 action in the uterus for up to 4 days. Because LY117018 has a shorter duration of action than monohydroxytamoxifen, a high dosage ratio of LY117018 over monohydroxytamoxifen is required to maintain effective competitive antagonism in the uterus. Overall, these findings suggest that monohydroxytamoxifen and LY117018 probably act through the same mechanism of action via the estrogen receptor.

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药物靶点

药物	目标	类	生物	药理作用	行动
Chlorotrianisene	雌激素受体α	蛋白质	人类	是的	受体激动剂	细节