Stimulation of Adenosine 3',5'-monophosphate formation in incubated rat hypothalamus by estrogenic compounds: relationship to biologic potency and blockade by anti-estrogens.
Several estrogenic compounds were examined for their abilities to stimulate the formation of adenosine 3',5'-monophosphate (cyclic AMP) in incubated hypothalami from immature (27-28 day old) female rats. 17-beta estradiol (E2) and diethylstilbestrol (DES) significantly increased the formation of cyclic AMP while estrone and estriol elicited small but not statistically significant increases in cyclic AMP formation. 17-alpha estradiol was ineffective in increasing cyclic AMP formation. The anti-estrogenic agent clomiphene was found to effectively antagonize the formation of cyclic AMP elicited by E2 and DES, while having no stimulatory effects  on cyclic AMP formation itself. These data indicate that the binding of estrogenic compounds to cytoplasmic sites (receptors) in the hypothalamus is required for subsequent stimulation of cyclic AMP formations.
D000818:Animals; D002996:Clomiphene / Q000494:pharmacology; D000242:Cyclic AMP / Q000096:biosynthesis*; D004054:Diethylstilbestrol / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004958:Estradiol / Q000494:pharmacology*; D004964:Estriol / Q000494:pharmacology; D004970:Estrone / Q000494:pharmacology; D005260:Female; D007031:Hypothalamus / Q000187:drug effects / Q000378:metabolism*; D009638:Norepinephrine / Q000494:pharmacology; D051381:Rats
D002996:Clomiphene; D004970:Estrone; D004958:Estradiol; D004054:Diethylstilbestrol; D000242:Cyclic AMP; D004964:Estriol; D009638:Norepinephrine