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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Bibliographic Details
Published in:Neuroscience 2015-04, Vol.290, p.138-146
Main Authors: Rey, M, Veleiro, A.S, Ghini, A.A, Kruse, M.S, Burton, G, Coirini, H
Format: Article
Language:English
Subjects:
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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Summary: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