Non-benzodiazepine, Ag-dependent, brain-specific binding sites for [3H]beta-carboline-3-carboxylic acid ethyl ester.
Specific, saturable and reversible binding of [3H]beta + CCE ([3H]beta-carboline-3-carboxylic acid ethyl ester) in buffer containing 20 microM AgNO3 and 10 microM diazepam was detected in rat brain membranes. The binding of [3H]beta CCE to non-benzodiazepine binding sites is Ag+ (Cu)-dependent, stimulated by NaCl and ascorbic acid and inhibited by dithiothreitol. The concentration of non-benzodiazepine [3H]beta CCE binding sites (Bmax) determined in the brain membranes was 1180 +/- 320 pmol/g tissue, and Kd = 77 +/- 19 nM. [3H]beta CCE bound to benzodiazepine receptors in the same membranes with Bmax = 81 +/- 9 pmol/g tissue and Kd = 3.2 +/- 0.4 nM.
Korneyev AYa
Institute of Pharmacology, Acad. Med. Sci. U.S.S.R., Moscow.
Meliksetyan
M B
MB
D000818:Animals; D001665:Binding Sites; D001921:Brain / Q000378:metabolism*; D002243:Carbolines / Q000378:metabolism*; D003975:Diazepam / Q000494:pharmacology; D005445:Flunitrazepam / Q000494:pharmacology; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D008566:Membranes / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D011963:Receptors, GABA-A / Q000187:drug effects / Q000378:metabolism; D012834:Silver / Q000378:metabolism*
D002243:Carbolines; D011963:Receptors, GABA-A; D012834:Silver; D005445:Flunitrazepam; C024915:beta-carboline-3-carboxylic acid ethyl ester; D003975:Diazepam