Benzodiazepines stimulate muscimol receptor binding in an Ro 15-1788 reversible manner.
Diazepam and other benzodiazepines caused a concentration-dependent increase of [3H]muscimol (15 nM) specific binding. The maximal increase was 23.6 +/- 5% at the diazepam concentration of 10 microM. Concentrations of half-maximal stimulation for diazepam and clonazepam were 43 +/- 17 and 12.6 +/- 6 nM respectively. Ro 15-1788 was found to inhibit the stimulation of muscimol specific binding induced by other benzodiazepines. The IC50 for diazepam (1000 nM)-induced stimulation was 280 +/- 60 nM. Intensive treatment of membranes with Triton X-100 decreased the stimulatory effect of benzodiazepines.
D000818:Animals; D001569:Benzodiazepines / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D001570:Benzodiazepinones / Q000494:pharmacology*; D001921:Brain / Q000378:metabolism; D002122:Calcium Chloride / Q000494:pharmacology; D005442:Flumazenil; D066298:In Vitro Techniques; D008297:Male; D008566:Membranes / Q000378:metabolism; D017830:Octoxynol; D011092:Polyethylene Glycols / Q000494:pharmacology; D011189:Potassium Chloride / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011956:Receptors, Cell Surface / Q000187:drug effects* / Q000378:metabolism; D011963:Receptors, GABA-A
D001570:Benzodiazepinones; D011956:Receptors, Cell Surface; D011963:Receptors, GABA-A; D001569:Benzodiazepines; D011092:Polyethylene Glycols; D005442:Flumazenil; D011189:Potassium Chloride; D017830:Octoxynol; D002122:Calcium Chloride