Bennett D R, Debono M, Powell J G, Rathmacher R P, Cochrane R L
J Endocrinol Invest. 1982 Jul-Aug;5(4):223-6. doi: 10.1007/BF03348327.
The compound 17 cyano-5,16 androstadien-3 beta-ol-acetate (cyanoacetate) was considered as a promising candidate for use as a contraceptive agent, since it was reported to specifically inhibit the ovarian conversion of pregnenolone to progesterone. A preliminary study in rats indicated that this compound had unique properties that interfered with the interpretation of results concerning the decidual response. It appeared to interact with the ovaries of the animal to cause an increase in uterine weight. Because of these observations, a multiple factorial study was designed to determine whether this compound was, in fact, more uterotrophic in intact, than in spayed, psuedopregnant rats. The study demonstrated that the presence of the ovary resulted in a significantly greater uterine weight, while 2 mg progesterone daily for 10 days had no significant effect on uterine weight. Cyanoacetate (10 mg/day for 10 days) was found to increase uterine weight significantly in intact, but not spayed, psuedopregnant rats. Neither cyanoacetate (10 mg/day) nor progesterone (2 mg/day) affected ovarian weight. The data suggest that cyanoacetate is converted by the ovary from a compound with little uterotrophic activity to a material with substantial uterotrophic activity.
化合物17 - 氰基 - 5,16 - 雄甾二烯 - 3β - 醇 - 醋酸酯(氰基醋酸酯)被认为是一种有前景的避孕药物候选物,因为据报道它能特异性抑制孕烯醇酮向孕酮的卵巢转化。在大鼠身上进行的一项初步研究表明,该化合物具有独特的性质,干扰了关于蜕膜反应结果的解读。它似乎与动物的卵巢相互作用,导致子宫重量增加。基于这些观察结果,设计了一项多因素研究,以确定该化合物在完整的假孕大鼠中是否实际上比在摘除卵巢的假孕大鼠中更具有子宫营养作用。研究表明,卵巢的存在导致子宫重量显著增加,而每天注射2毫克孕酮,持续10天,对子宫重量没有显著影响。发现氰基醋酸酯(每天10毫克,持续10天)能使完整的假孕大鼠子宫重量显著增加,但对摘除卵巢的假孕大鼠则无此作用。氰基醋酸酯(每天10毫克)和孕酮(每天2毫克)均未影响卵巢重量。数据表明,氰基醋酸酯被卵巢从一种子宫营养活性较低的化合物转化为一种具有显著子宫营养活性的物质。