3- (1-Iminoethyl) -4,5-cycloalkylpyridine-2,6-diol derivatives. a novel class of benzodiazepine receptor antagonists and partial agonists
Barone, D.; Colombo, G.; Gallico, L.; Winters, G.; Sala, A.; Tarzia, G.
Il Farmaco; Edizione Scientifica 42(11): 845-859
1987
ISSN/ISBN: 0430-0920 PMID: 2832209 Document Number: 299958
A series of 3-(1-iminoethyl)-4,5-cycloalkylpyridine-2,6-diol derivatives have been prepared from isoxazolo [5,4-b] pyridones. Some of these compounds had affinity for the benzodiazepine receptors in vitro and in vivo radioligand displacement assays. These compounds did not have any anticonvulsant properties and were not active in pharmacological tests predictive of antianxiety activity, but antagonised the anticonvulsant and muscle-relaxant effects of diazepam and had proconvulsant properties.