Biol. Chem. Hoppe-Seyler Vol. 374, pp. 265-270, April 1993 Astrid JUSSOFIE Institut f r Physiologische Chemie, Universit tsklinikum Essen (Received 20 November 1992/24 February 1993) Summary: The allosteric regulation of specific [3H]muscimol binding by neuroactive steroids to the GABA-binding sites of membrane fractions prepared from five different brain areas was characterized in order to elucidate if the regionally variable subunit composition of GABAA receptors is reflected in the responsiveness of the GABA binding site to neurosteroid modulatory effects. At a final concentration of , progesterone and its metabolite 3-a-hydroxy-5a-pregnane-20-one (HPO) reduced the affinity in hippocampus (HIP), enhanced it in medulla (MED) and did not affect it in cerebellum (CER). However, there are differences in potency of these two steroids between frontal cortex (FC) and hypothalamus (HYP), since the affinity was enhanced in FC only by progesterone and in HYP only by HPO. While the magnitude of progesterone-induced alterations in affinity were similar in FC, MED and HIP, HPO affected the affinity significantly stronger in HIP than in HYP and MED. Concerning the density of the bind- ing sites progesterone exerted no significant modulatory effect in contrast to HPO which increased the number of binding sites (5max) in all
Biological Chemistry Hoppe-Seyler – de Gruyter
Published: Jan 1, 1993
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