Characteristics of [3H] propyl beta-carboline-3-carboxylate binding to benzodiazepine receptors in human brain.
Characterization of the binding of derivatives of beta-carboline-3-carboxylate, a putative endogenous ligand for benzodiazepine (BZ) receptors, has not previously been attempted in normal human brain. In the present study, we demonstrated saturable, high affinity binding of [3H] propyl beta-carboline-3-carboxylate [3H] PrCC) in normal human frontal cerebral cortex and cerebellum exhibiting pharmacological specificity similar to [3H] diazepam and [3H] flunitrazepam binding. The binding of [3H] PrCC is increased by chloride and GABA, but decreased by divalent cations, especially calcium. The profile of [3H] PrCC binding in human brain reflects specific interaction with BZ/ionophore/GABA receptor complexes.
D001667:Binding, Competitive / Q000187:drug effects; D002243:Carbolines / Q000378:metabolism*; D002413:Cations, Divalent / Q000494:pharmacology; D002531:Cerebellum / Q000378:metabolism*; D002540:Cerebral Cortex / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D005260:Female; D006219:Halogens / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D007211:Indoles / Q000378:metabolism*; D008297:Male; D009118:Muscimol / Q000494:pharmacology; D011956:Receptors, Cell Surface / Q000378:metabolism*; D011963:Receptors, GABA-A; D005680:gamma-Aminobutyric Acid / Q000494:pharmacology
D002243:Carbolines; D002413:Cations, Divalent; D006219:Halogens; D007211:Indoles; D011956:Receptors, Cell Surface; D011963:Receptors, GABA-A; D009118:Muscimol; D005680:gamma-Aminobutyric Acid; C028585:propyl beta-carboline-3-carboxylate