The neuroactive steroid 3 alpha-hydroxy-5 beta-pregnan-20-one is a two-component modulator of ligand binding to the GABAA receptor

Neuroactive steroids allosterically inhibit [35S]t-butylbicyclophosphorothionate ([35S]TBPS) and enhance [3H]flunitrazepam binding to the GABAA receptor complex. In the presence of 5 microM GABA, 3 alpha-hydroxy-5 beta-pregnan-20-one (3 alpha, 5 beta-P) inhibits [35S]TBPS binding with high- (IC50 21...

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Veröffentlicht in:	European journal of pharmacology 1994-10, Vol.269 (2), p.157-163
Hauptverfasser:	Hawkinson, J E, Kimbrough, C L, McCauley, L D, Bolger, M B, Lan, N C, Gee, K W
Format:	Artikel
Sprache:	eng
Schlagworte:	20-alpha-Dihydroprogesterone - analogs & derivatives 20-alpha-Dihydroprogesterone - pharmacology Animals Brain Chemistry - drug effects Bridged Bicyclo Compounds - metabolism Bridged Bicyclo Compounds, Heterocyclic Cattle Cerebellum - drug effects Cerebellum - metabolism Convulsants - metabolism Flunitrazepam - metabolism Hippocampus - drug effects Hippocampus - metabolism In Vitro Techniques Ligands Male Membranes - drug effects Membranes - metabolism Receptors, GABA-A - drug effects Receptors, GABA-A - metabolism Thalamus - drug effects Thalamus - metabolism
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