New tricyclic enamine derivatives with CNS depressant properties.
63 tricyclic enamine derivatives were synthetized and pharmacologically tested. Many of the screened compounds showed remarkable CNS depressant chlorpromazine-like activities. The compounds no. 9 (substituents CH3, Cl, H), 18 (substituents CH3, F, H) and 27 substituents CH3, OCH3, H) resulted the most interesting and were studied in comparison with chlorpromazine and chlordiazepoxide. They were submitted to further studies in view of trials in humans.
D000700:Analgesics / Q000494:pharmacology; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D001831:Body Temperature / Q000187:drug effects; D002490:Central Nervous System / Q000187:drug effects*; D003864:Depression, Chemical; D003986:Dibenzocycloheptenes / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D004353:Drug Evaluation, Preclinical; D006993:Hypnotics and Sedatives / Q000494:pharmacology; D007249:Inflammation / Q000188:drug therapy; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009125:Muscle Relaxants, Central / Q000494:pharmacology; D010879:Piperazines / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D013329:Structure-Activity Relationship
D000700:Analgesics; D003986:Dibenzocycloheptenes; D006993:Hypnotics and Sedatives; D009125:Muscle Relaxants, Central; D010879:Piperazines