NNC45-0781是一种组织选择性的雌激素(estrogen)部分激动剂。
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NNC45-0781 is a tissue-selective estrogen partial-agonist.
NNC45-0781 (NNC 45-0781) shows that it is a very promising tissue-selective estrogen agonist. Total serum cholesterol is significantly increased in the vehicle-treated group as compared to the sham animals. All of the animals receiving NNC45-0781 at doses of 10 nmol/g or higher, has significantly lower levels of total serum cholesterol as compared to the vehicle treated group[1].
[1]. Bury PS, et al. Synthesis and pharmacological evaluation of novel cis-3,4-diaryl-hydroxychromanes as high affinity partial agonists for the estrogen receptor. Bioorg Med Chem. 2002 Jan;10(1):125-45.
Animal experiment: | Rats[1]Female Sprague-Dawley rats, 12 weeks of age, weighing approximately 250 g are used in these studies.The pharmacological properties of NNC45-0781 (NNC 45-0781) are studied through a series of in vivo experiments. Activity of orally administered NNC45-0781 (1,10, 50 and 100 nmol/g) on total serum cholesterol in the ovariectomized rat. |
参考文献: [1]. Bury PS, et al. Synthesis and pharmacological evaluation of novel cis-3,4-diaryl-hydroxychromanes as high affinity partial agonists for the estrogen receptor. Bioorg Med Chem. 2002 Jan;10(1):125-45. |
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