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RU486,17β-羟-11β-(4-α甲基胺苯1)-17α(丙-1-炔基)-酯-4,9-2烯-3-酮,是一种炔诺酮的衍生物,是在孕激素C17α上加一个侧链,再在C11β上加一个外环逐步合成的孕激素类。C17α上的侧链可能对增加受体的亲和力有关。而C11β的外环与抗雌激素类似,可能与受体失活有关。显然,RU486除了对孕酮受体有非常高的亲和力外,也能结合于糖皮质类固醇受体。RU486确也是一种糖皮质类固醇拮抗剂,并可能有其它的治疗用途。不过,这不会影响它用于女性控制生育。RU486对雄激素受体也有一定的亲和力,并有一定的抗雄激素能力。同样,这也不影响它用作抗孕药。RU486既不是雌激素,也不是抗雌激素;既不是糖皮质类固醇或盐皮质类固醇的促效剂,也不是盐皮质类固醇拮抗剂。
RU486, 17β-hydroxy-11β- (4-α-methylamine benzene 1) -17α (prop-1-ynyl) -ester-4,9-2-en-3-one is a derivative of norethindrone The substance is added with a side chain on the progestin C17α, followed by a stepwise synthesis of the progestin on the C11β. Side chains on C17α may be involved in increasing receptor affinity. The outer ring of C11β is similar to antiestrogen, which may be related to the receptor inactivation. Obviously, RU486, in addition to having a very high affinity for progesterone receptors, can also bind to glucocorticosteroid receptors. RU486 is indeed a glucocorticosteroid antagonist and may have other therapeutic uses. However, this does not affect it for female control of childbirth. RU486 also has some affinity for androgen receptor, and has some anti-androgenic ability. Again, this does not affect its use as an anti-infective. RU486 is neither estrogen nor anti-estrogen; nor is it an agonist of glucocorticoid or corticosteroid, nor is it a mineralocorticoid antagonist.