Chronic exposure to a benzodiazepine partial agonist does not alter GABAA receptor function in cultured neurons.
The benzodiazepine partial agonist Ro16-6028 does not lead to GABAA receptor downregulation in vivo. To assess effects of this compound in vitro, cultured neurons were exposed to Ro16-6028, 1 and 10 microM. GABA-dependent chloride uptake was unaffected at either dose of Ro16-6028 from 2 to 10 days, in contrast to decreased function observed with clonazepam, 1 microM, at 10 days, Ro16-6028 exposure did not alter GABA-independent chloride uptake, total neuronal protein, or cellular protein synthesis.
Miller
L G
LG
Department of Psychiatry, Tufts University School of Medicine, Boston, MA.
Heller
J
J
D000818:Animals; D001570:Benzodiazepinones / Q000494:pharmacology*; D002478:Cells, Cultured; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D002642:Chick Embryo; D002712:Chlorides / Q000378:metabolism; D002998:Clonazepam / Q000494:pharmacology; D015536:Down-Regulation / Q000187:drug effects; D008715:Methionine / Q000378:metabolism; D009419:Nerve Tissue Proteins / Q000378:metabolism; D009474:Neurons / Q000187:drug effects / Q000378:metabolism*; D011963:Receptors, GABA-A / Q000187:drug effects*; D013462:Sulfur Radioisotopes
D001570:Benzodiazepinones; D002712:Chlorides; D009419:Nerve Tissue Proteins; D011963:Receptors, GABA-A; D013462:Sulfur Radioisotopes; D002998:Clonazepam; D008715:Methionine; C054626:bretazenil