Diazepam receptors on mouse astrocytes in primary cultures: displacement by pharmacologically active concentrations of benzodiazepines or barbiturates.
Astrocytes in primary cultures were found to bind large amounts of [3H]diazepam. More than 90% of the total binding is specific, i.e., displaceable by an excess of nonlabeled diazepam. At saturation the specific binding amounts to about 20 pmol/mg protein and the Kd value is 30 nM. Clonazepam and flurazepam displace [3H]diazepam from its specific binding sites; 20-30% displacement is brought about by 0.1-0.3 microM clonazepam, which is similar to the plasma concentrations encountered in epileptic patients treated with this drug. Barbiturates have a similar effect, but considerably higher concentrations are required.
D000818:Animals; D001253:Astrocytes / Q000378:metabolism*; D001463:Barbiturates / Q000378:metabolism*; D001569:Benzodiazepines / Q000378:metabolism*; D001665:Binding Sites; D001667:Binding, Competitive; D002478:Cells, Cultured; D002998:Clonazepam / Q000378:metabolism; D003975:Diazepam / Q000378:metabolism*; D005479:Flurazepam / Q000378:metabolism; D051379:Mice; D010424:Pentobarbital / Q000378:metabolism; D010634:Phenobarbital / Q000378:metabolism; D011955:Receptors, Drug / Q000378:metabolism*
D001463:Barbiturates; D011955:Receptors, Drug; D001569:Benzodiazepines; D002998:Clonazepam; D010424:Pentobarbital; D005479:Flurazepam; D003975:Diazepam; D010634:Phenobarbital