Abstract
The β-carbolines, which are potent ligands for benzodiazepine receptors, antagonize the pharmacological actions of benzodiazepines. In the cat, the stable β-carboline derivative methylamide-β-carboline-3-carboxylate, FG 7142, and the specific benzodiazepine antagonist Ro 15-1788 reversed behavioral and electroencephalographic (EEG) changes produced by a single dose of diazepam. Surprisingly, the β-carboline did not elicit signs of withdrawal when given after 22 days of a daily dose regimen of diazepam, while Ro 15-1788 precipitated an acute abstinence syndrome largely characterized by tremors, increased muscle tone, back arching, myoclonic jerks and pupil dilatation. Unlike Ro 15-1788, the β-carboline produced effects of its own such as behavioral states of arousal and fearfulness. These findings indicate that the β-carboline functionally interacts with benzodiazepine receptors in a manner unlike that seen with typical agonists and antagonists.
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Ongini, E., Marzanatti, M., Bamonte, F. et al. A β-carboline antagonizes benzodiazepine actions but does not precipitate the abstinence syndrome in cats. Psychopharmacology 86, 132–136 (1985). https://doi.org/10.1007/BF00431697
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DOI: https://doi.org/10.1007/BF00431697