Structure-activity relationship studies of CNS agents. Part 4: 2-[3-(4-aryl-1-piperazinyl)propyl]-1,2,3,4-tetrahydro-beta-carbolin+ ++ -1-one derivatives as potential central anti-serotonin agents.
Seven derivatives of 1,2,3,4-tetrahydro-beta-carbolin-1-one have been prepared. Three of them showed significant central anti-serotonin activity, comparable with that of trazodone or etoperidone. Some structural features were found to be important for the central antiserotonin activity of the investigated class of compounds.
Boksa
J
J
Institute of Pharmacology, Polish Academy of Sciences, Kraków.
Misztal
S
S
Chojnacka-Wójcik
E
E
Gastoł-Lewińska
L
L
Gródecka
A
A
Mokrosz
J L
JL
D006916:5-Hydroxytryptophan / Q000037:antagonists & inhibitors; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D002243:Carbolines / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D008297:Male; D051379:Mice; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D002243:Carbolines; D010879:Piperazines; D012702:Serotonin Antagonists; D006916:5-Hydroxytryptophan