3-(1-Iminoethyl)-4,5-cycloalkylpyridine-2,6-diol derivatives. A novel class of benzodiazepine receptor antagonists and partial agonists.
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.
Barone
D
D
Department of Pharmacology, Lepetit Research Laboratories, Milano, Italy.
Colombo
G
G
Gallico
L
L
Winters
G
G
Sala
A
A
Tarzia
G
G
D000818:Animals; D001640:Bicuculline / Q000494:pharmacology; D001667:Binding, Competitive; D055598:Chemical Phenomena; D002621:Chemistry; D005445:Flunitrazepam / Q000378:metabolism; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D051379:Mice; D009125:Muscle Relaxants, Central; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D011919:Rats, Inbred Strains; D011963:Receptors, GABA-A / Q000187:drug effects*
D009125:Muscle Relaxants, Central; D011725:Pyridines; D011963:Receptors, GABA-A; D005445:Flunitrazepam; D001640:Bicuculline