Cano A, Morcillo N, Lopez F, Marquina P, Parrilla J J, Abad L
Eur J Obstet Gynecol Reprod Biol. 1986 Apr;21(4):245-52. doi: 10.1016/0028-2243(86)90024-9.
Danazol, testosterone and dihydrotestosterone (DHT) were tested as competitors for estrogen receptors on immature rat uterus cytosol. No competitive binding could be demonstrated for any of these steroids. After that, prepubertal Wistar rats were exposed to danazol, testosterone or propylene glycol (control) for 3 days or 17 days. After the appropriate exposure to medication, the animals were killed. Both danazol and testosterone appeared to be uterotropic after 3 days of treatment, although the increase in the uterine weight was significant only in the danazol-treated group (p less than 0.05). This effect was lost after 17 days of treatment. Estradiol receptor binding assays were done on the cytosolic and nuclear fractions of the homogenized uterine tissue of each group. The estrogen binding capacity of cytosols was increased in both the danazol (p less than 0.05) and the testosterone (p less than 0.01) groups after 3 days of treatment. A parallel increase was found in the nuclear fraction of both groups. After 17 days of treatment, the comparison between the 3 groups showed no differences in the cytosolic or nuclear estrogen binding capacity. The information provided by this study suggests that some effects of danazol may be due to an androgenic action and that may be associated to increases in the free fraction of testosterone.
将达那唑、睾酮和双氢睾酮(DHT)作为未成熟大鼠子宫胞浆中雌激素受体的竞争剂进行了测试。这些类固醇均未显示出竞争性结合。此后,将青春期前的Wistar大鼠暴露于达那唑、睾酮或丙二醇(对照)中3天或17天。在适当暴露于药物后,处死动物。治疗3天后,达那唑和睾酮似乎都具有促子宫生长作用,尽管仅在达那唑治疗组子宫重量增加显著(p小于0.05)。治疗17天后这种作用消失。对每组匀浆子宫组织的胞浆和核部分进行雌二醇受体结合测定。治疗3天后,达那唑组(p小于0.05)和睾酮组(p小于0.01)的胞浆雌激素结合能力均增加。两组的核部分也有平行增加。治疗17天后,三组之间的比较显示胞浆或核雌激素结合能力无差异。本研究提供的信息表明,达那唑的某些作用可能归因于雄激素作用,并且可能与睾酮游离部分的增加有关。