[Selection of preparations with anticipated antiestrogen activity].
Specificity of interaction between estrogen-receptor systems of guinea pig uterus and oviducts and six estrogens was studied. The obtained datas suggest existence of tissue specificity in estrogen-receptor interaction in uterus and oviducts. Modifications of the steroid molecule led to decrease in extent of estrogen affinity. Introduction of an ethyl group into 17 alpha-position resulted in the effect, by the rate of estrogen-receptor binding equal to reduction of 17 beta-hydroxyl. Low but distinct affinity of 17 alpha-estradiol, its structure and stability, enabled to select this substance as a preparation with anticipated anti-estrogenic activity.
D000345:Affinity Labels / Q000494:pharmacology; D000818:Animals; D003600:Cytosol / Q000187:drug effects; D004962:Estranes / Q000494:pharmacology; D004965:Estrogen Antagonists / Q000494:pharmacology*; D005187:Fallopian Tubes / Q000187:drug effects; D005260:Female; D006168:Guinea Pigs; D011960:Receptors, Estrogen / Q000187:drug effects; D013329:Structure-Activity Relationship; D014599:Uterus / Q000187:drug effects
D000345:Affinity Labels; D004962:Estranes; D004965:Estrogen Antagonists; D011960:Receptors, Estrogen
Otbor preparatov s prepolagaemoĭ antiéstrogennoĭ aktivnost'iu.