Английская Википедия:DU-41165

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DU-41165, also known as 6-fluoro-16-methylene-17α-acetoxy-δ6-retroprogesterone, is a progestin which was developed by Philips-Duphar in the 1970s and was never marketed.[1][2] It is a combined derivative of 17α-hydroxyprogesterone and retroprogesterone.[1][2] The drug shows extremely high potency as a progestogen in animals.[1] It has been found to possess 158% of the relative binding affinity of promegestone for the progesterone receptor expressed in rat uterus (relative to 74% for the closely related progestin DU-41164).[1] DU-41165 also showed 28% of the affinity of RU-28362 for the glucocorticoid receptor expressed in rat liver, but no affinity for the mineralocorticoid receptor expressed in rat kidney (<0.003% of that of RU-26752).[1] The drug showed no androgenic, anabolic, or estrogenic activity in animals, but did show some antiandrogenic and glucocorticoid activity at high doses.[1] Although highly potent in animals, DU-41165 produced little or no progestogenic effect at dosages of 50 and 200 µg/day in women, suggesting major species differences.[1] DU-41165 has been studied as a potential photoaffinity label for the progesterone receptor.[1]

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Шаблон:Androgen receptor modulators Шаблон:Glucocorticoid receptor modulators Шаблон:Progesterone receptor modulators

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  1. ↑ 1,0 1,1 1,2 1,3 1,4 1,5 1,6 1,7 Шаблон:Cite journal
  2. ↑ 2,0 2,1 Шаблон:Cite journal
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