Estrogen modulation of the gamma-aminobutyric acid receptor complex in the central nervous system of rat.
Administration of estradiol benzoate to ovariectomized rats results in an increased binding of [3H]muscimol, [3H]diazepam and 35S-t-butylbicyclophosphorothionate in various areas of the central nervous system of rats. The effect is dose-dependent and its onset can be observed as early as 12 hr after s.c. administration of the hormone. The various binding activities are differentially affected by the hormonal treatment: the maximal effect observed for [3H]diazepam binding is in the cerebellum (+42%), for [3H]muscimol binding in the frontal cortex (+84%) and for 35S-t-butylbicyclophosphorothionate binding in the striatum (+46%) indicating that the activities of the sites are not under the same cellular regulatory control. The estrogen-induced increase in [3H]diazepam binding sites does not result in an increased protection against chemoconvulsants such as pentylenetetrazole.
Perez
J
J
Milano Molecular Pharmacology Lab, University of Milan, Italy.
Zucchi
I
I
Maggi
A
A
D000818:Animals; D001921:Brain / Q000187:drug effects*; D001643:Bridged Bicyclo Compounds / Q000378:metabolism; D019086:Bridged Bicyclo Compounds, Heterocyclic; D003975:Diazepam / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004967:Estrogens / Q000494:pharmacology*; D005260:Female; D009118:Muscimol / Q000494:pharmacology; D012313:RNA / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D011963:Receptors, GABA-A / Q000187:drug effects*; D012640:Seizures / Q000139:chemically induced
D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D004967:Estrogens; D011963:Receptors, GABA-A; D009118:Muscimol; D012313:RNA; C037476:tert-butylbicyclophosphorothionate; D003975:Diazepam