Selective, partial agonist for the benzodiazepine binding site of the GABAA
receptor. Potently inhibits [3H]-flunitrazepam binding to central benzodiazepine receptors (IC50
= 1.3 nM) and displays weak affinity for peripheral benzodiazepine (IC50
= 0.68 - 2.25 μ
M) and GABA binding sites (IC50
> 10000 μ
M). Displays anxiolytic activity in vivo
following oral administration.�.
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Pharmacology of the pyrazolo-type compounds: agonist, antagonist and inverse agonist actions.
CGS 20625, a novel pyrazolopyridine anxiolytic.
Williams et al.
CGS 20625, a novel pyrazolopyridine with selective anxiolytic activity.
Jarvis et al.