A quantitative structure-activity relationship study on some pyrazolo[4,5-c]quinolines acting as inhibitors of benzodiazepine-receptor binding.

By a quantitative structure-activity relationship (QSAR) study, the ability of a series of 1-arylpyrazolo[4,5-c]quinolin-4-ones to displace specific [3H]-flunitrazepam from bovine brain membranes is shown to be significantly correlated with steric and hydrophobic constants of aryl subtituents, suggesting that substituents of 2- and 6-positions produce dominant steric effects and that those of 3- and 5-positions are involved in strong hydrophobic interaction with the receptor.