Henry E C, Miller R K
Teratology. 1986 Aug;34(1):59-63. doi: 10.1002/tera.1420340108.
LY117018 (LY) has high affinity for the adult rat uterine estrogen receptor, has little uterotrophic activity, and inhibits many estradiol (E2)-induced responses in the adult or immature uterus. In these studies, LY was injected into day 19 rat fetuses, with and without diethylstilbestrol (DES) or E2, to determine whether it could block the estrogen-induced teratogenesis. LY at 1, 25, or 50 micrograms/fetus failed to decrease the 15-70% incidences of oviduct malformation and cleft phallus induced by DES (2.5 micrograms/fetus) or E2 (50 micrograms/fetus). However, LY alone (1-50 micrograms/fetus) was more potent than E2 in eliciting these same urogenital malformations. LY also failed to compete in vitro for plasma protein-bound 3H-E2, and therefore, like DES, is more available than E2 for uptake into fetal tissues. Thus, in the fetus, unlike the adult, LY was an estrogen agonist, which indicates that the fetus has a very different sensitivity than the adult to estrogenic compounds.
LY117018（LY）对成年大鼠子宫雌激素受体具有高亲和力，子宫营养活性低，并能抑制成年或未成熟子宫中许多雌二醇（E2）诱导的反应。在这些研究中，将LY注射到第19天的大鼠胎儿体内，同时给予或不给予己烯雌酚（DES）或E2，以确定它是否能阻断雌激素诱导的致畸作用。每只胎儿注射1、25或50微克的LY未能降低由DES（每只胎儿2.5微克）或E2（每只胎儿50微克）诱导的15 - 70%的输卵管畸形和阴茎裂的发生率。然而，单独使用LY（每只胎儿1 - 50微克）在引发这些相同的泌尿生殖系统畸形方面比E2更有效。LY在体外也不能与血浆蛋白结合的3H - E2竞争，因此，与DES一样，比E2更容易被胎儿组织摄取。因此，在胎儿中，与成年个体不同，LY是一种雌激素激动剂，这表明胎儿对雌激素化合物的敏感性与成年个体非常不同。
