Effect of synthetic steroids on GABAA receptor binding in rat brain

• Published in: Neuroscience Vol. 290; pp. 138 - 146
• Main Authors: Rey, M, Veleiro, A.S, Ghini, A.A, Kruse, M.S, Burton, G, Coirini, H
• Format: Journal Article
• Language: English
• Published: United States Elsevier Ltd 02-04-2015
• 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; CC; SS; muscimol; hippocampus; GABA A receptor; autoradiography; neurosteroids; MUS; L-Mol; t-butyl-bicyclophosphorothionate; FLU; cerebral cortex; synthetic steroids; TBPS; HC; stratum radiatum lacunosum moleculare layer; flunitrazepam; GABAA receptor; GABA(A) receptor
• ISSN: 0306-4522; 1873-7544
• DOI: 10.1016/j.neuroscience.2014.12.082

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.