Abstract
β-Carboline-3-carboxylic acid ethyl ester (β-CEE) displaced [3H]flunitrazepam from the mouse brain benzodiazepine receptor in vivo with an i.v. ED50 of 2.1 mg/kg, an i.p. ED50 and 53.4 mg/kg, and an i.g. ED50 of 450 mg/kg. At 2.1 mg/kg i.v. β-CEE displaced 37 ± 9% of the label from hippocampal membranes and 76 ± 7% from cerebellar membranes. The results suggest that the in vitro binding specificity of β-CEE is also expressed in vivo and that the drug may act in vivo by binding to the benzodazepine receptor.
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