Proceedings of the National Academy of Sciences · 1983 · 217 citations · 21 references
MedicineNeurosciencePharmacologyBehavioral PharmacologyNeuropharmacologyPsychopharmacologyAnxiolytic PharmacologyMechanisms Of Drug ActionAntagonistic InteractionsAnxiolytic ActionBenzodiazepine AntagonismBenzodiazepine Receptor AgonistsGamma-aminobutyric Acid ModulatorsGamma-aminobutyric Acid Receptor Modulation
By using Vogel's method to test the anxiolytic action of benzodiazepines and reducing the intensity of the current delivered to the drinking tube, it is possible to distinguish the pharmacological activity of three types of ligands for the benzodiazepine recognition site. An anticonflict action typical of anxiolytic benzodiazepines, a proconflict action typical of many beta-carbolines, including FG 7142 (beta-carboline-3-carboxylic acid ethyl ester methyl amide), and an antagonistic action of the proconflict and anticonflict actions typical of RO 15-1788 (ethyl-8-fluoro-5, 6-dihydro-5-methyl-6-oxo-4H-imidazol[1,5-alpha]-[1, 4]-benzodiazepine-3-carboxylate) and CGS 8216 (2-phenylpyrazolo[4,3-c]quinolin-3-(5H)-one). Pentylenetetrazole, which causes convulsions by interacting with a subunit of the gamma-aminobutyric acid receptor that is different from the benzodiazepine recognition site, also induces a proconflict action that is antagonized by anxiolytic benzodiazepines but not by RO 15-1788.
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Selective antagonists of benzodiazepines
Walter Hunkeler, H. Möhler, L. Pieri et al. · Nature · 1981 · 1.2K citations
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John F. Tallman, John W. Thomas, Dorothy W. Gallager · Nature · 1978 · 725 citations
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Interaction of Convulsive Ligands with Benzodiazepine Receptors
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Agonist and antagonist benzodiazepine receptor interaction in vitro
H. Möhler, J. G. Richards · Nature · 1981 · 381 citations