CGS 9895 is a GABA antagonist that acts via the benzodiazepine binding site of ag containing GABA receptors. CGS 9895 is the only known compound that can specifically enhance GABA-induced currents in ab subunit containing receptors, and acts at the extracellular a1+b3- subunit interface.
CGS 9895 is a GABA antagonist; GABAA receptor selective enhancer.
Several categories of compounds active at benzodiazepine receptors (BZR) in the brain have been distinguished: agonists, antagonists and the novel category of inverse agonist. In terms of their effects on ingestional responses (e.g., food, saline and water consumption), agonists increase
Rats were trained to respond under 3-min fixed-interval schedules of food presentation, and effects of the benzodiazepine-receptor ligands, flumazenil, 2-(4-methoxy-phenyl)-pyrazolo[4,3-c]quinolin-3(5H)-one (CGS 9895), 3-carbo-t-butoxy-beta-carboline (beta-CCtB), and beta-carboline-3-carboxylic acid ethyl ester (beta-CCE) were assessed before and after the induction of tolerance to
Pharmacology, biochemistry, and behavior, 23(2), 317-323 (1985-08-01)
The effects of diazepam and the pyrazoloquinoline benzodiazepine receptor ligands CGS8216, CGS9896, and CGS9895 on schedule-controlled responding were studied in dogs. Responding was maintained under a multiple fixed-interval (FI) 5-min fixed-ratio (FR) 30 response schedule of food presentation. Diazepam (PO)
The Journal of pharmacology and experimental therapeutics, 235(3), 589-595 (1985-12-01)
CGS 9895, a pyrazoloquinolone benzodiazepine receptor ligand, was administered alone and concomitantly with diazepam in order to assess its agonist and diazepam-antagonist properties on various behaviors in rodents. In mice, CGS 9895 neither potentiated nor blocked the convulsant effects of
European journal of pharmacology, 92(1-2), 155-157 (1983-08-19)
The diazepam-like agonist and diazepam antagonist properties of the pyrazoloquinoline benzodiazepine receptor ligands CGS8216, CGS9895 and CGS9896 were evaluated in rats trained to discriminate between saline and 1.0 mg/kg of diazepam in a two-choice, discrete-trial procedure. None of the three