Interactions of beta-carbolines with the benzodiazepine receptor: structure-activity relationships.
The effects of a number of beta-carboline derivatives on [3H]flunitrazepam binding to the benzodiazepine binding site were investigated. The potency of beta-carbolines at the benzodiazepine binding site appeared to be determined largely by the aromaticity of the molecule. Norharmane-3-carboxylic acid ethyl ester was considerably more potent (IC50 10 nM) than its tetrahydro-beta-carboline analogue (IC50 6 microM). There is essentially no difference in potency between the (+)- and (--)-forms of the tetrahydro-beta-carboline-3-carboxylate analogues.
D000818:Animals; D001665:Binding Sites; D002243:Carbolines / Q000494:pharmacology*; D005445:Flunitrazepam / Q000378:metabolism; D066298:In Vitro Techniques; D007211:Indoles / Q000494:pharmacology*; D051381:Rats; D011955:Receptors, Drug / Q000187:drug effects* / Q000378:metabolism; D011963:Receptors, GABA-A; D013329:Structure-Activity Relationship
D002243:Carbolines; D007211:Indoles; D011955:Receptors, Drug; D011963:Receptors, GABA-A; D005445:Flunitrazepam