Effect of synthetic steroids on GABAA receptor binding in rat brain

Highlights • GABAA receptor binding was tested using synthetic steroids with A/B ring low flexibility. • Three ligands for specific binding sites were tested by quantitative in vitro autoradiography. • Natural and synthetic steroids show different effect on the cerebral cortex and hippocampus. • The...

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Veröffentlicht in:	Neuroscience 2015-04, Vol.290, p.138-146
Hauptverfasser:	Rey, M, Veleiro, A.S, Ghini, A.A, Kruse, M.S, Burton, G, Coirini, H
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Autoradiography Binding, Competitive Bridged Bicyclo Compounds, Heterocyclic - chemistry Bridged Bicyclo Compounds, Heterocyclic - metabolism cerebral cortex Cerebral Cortex - drug effects Cerebral Cortex - metabolism Flunitrazepam - metabolism GABA-A Receptor Agonists - metabolism GABA-A Receptor Agonists - pharmacology GABAA receptor hippocampus Hippocampus - drug effects Hippocampus - metabolism Male Muscimol - metabolism Neurology neurosteroids Pregnanolone - analogs & derivatives Pregnanolone - chemistry Pregnanolone - metabolism Pregnanolone - pharmacology Protein Binding Rats, Sprague-Dawley Receptors, GABA-A - metabolism Sulfur Radioisotopes synthetic steroids Tritium
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Zusammenfassung:	Highlights • GABAA receptor binding was tested using synthetic steroids with A/B ring low flexibility. • Three ligands for specific binding sites were tested by quantitative in vitro autoradiography. • Natural and synthetic steroids show different effect on the cerebral cortex and hippocampus. • The 3α-hydroxy-6,19-epoxypregn-4-ene-20-one steroid may be used as allopregnanolone agonist.
ISSN:	0306-4522 1873-7544
DOI:	10.1016/j.neuroscience.2014.12.082