beta-Carboline inhibition of benzodiazepine receptor binding in vivo.
The in vivo potencies of 4 beta-carboline derivatives as inhibitors of benzodiazepine receptor binding were investigated. For all 4 derivatives maximal inhibition was seen within 2 min after i.v. application but decreased continuously for the next 20 min and after this time accounted for less than one-third of maximal inhibition. The in vivo potencies of the beta-carbolines as inhibitors of benzodiazepine receptor binding are much smaller than one would expect from their affinities measured in vitro. Thus, it is assumed than only a small portion of the i.v. dose reaches the brain.
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D002243:Carbolines / Q000494:pharmacology*; D002998:Clonazepam / Q000378:metabolism; D003975:Diazepam / Q000378:metabolism; D005445:Flunitrazepam / Q000378:metabolism; D007211:Indoles / Q000494:pharmacology*; D008297:Male; D009115:Muridae; D011955:Receptors, Drug / Q000187:drug effects* / Q000378:metabolism; D011963:Receptors, GABA-A
D002243:Carbolines; D007211:Indoles; D011955:Receptors, Drug; D011963:Receptors, GABA-A; D002998:Clonazepam; D005445:Flunitrazepam; D003975:Diazepam