Central nervous system active 5-oxo-1,4,5,6,7,8-hexahydrocinnolines.
Among a series of 5-oxo-1,4,5,6,7,8-hexahydrocinnolines examined for their CNS activity, 1-(2-diethylaminoethyl)-3-(p-fluorophenyl)-5-oxo-7,7-dimethyl-1,4,5,6,7,8-hexahydrocinnoline (23) and 1-(2-dimethylaminoethyl)-3-phenyl-5-oxo-7,7-dimethyl-1,4,5,6,7,8-hexahydrocinnoline (27) had sedative and anticonvulsant properties and were also acitve in tests used to characterize antidepressants. But their narrow safety margin precluded further follow-up studies. Derivatives 35-38 of 2-(omega-phenacyl)-3-hydrazino-5,5-dimethyl-2-cyclohexenone were active in tests used to characterize antidepressants and were weakly sedative but not anticonvulsant.
D000818:Animals; D001831:Body Temperature / Q000187:drug effects; D002490:Central Nervous System / Q000187:drug effects*; D003864:Depression, Chemical; D004295:Dihydroxyphenylalanine / Q000494:pharmacology; D004597:Electroshock; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D011724:Pyridazines / Q000138:chemical synthesis* / Q000494:pharmacology; D012110:Reserpine / Q000037:antagonists & inhibitors; D012640:Seizures / Q000517:prevention & control; D013329:Structure-Activity Relationship
D011724:Pyridazines; D004295:Dihydroxyphenylalanine; D012110:Reserpine