[Synthesis of metabolites of mosapramine. II. Synthesis of phenolic metabolites of mosapramine and their pharmacological activities].
Four phenolic metabolites of (+-)-3-chloro-5-[3-(2-oxo-1,2,3,5,6,7,8,8a-octahydroimidazo[1,2- a]pyridine-3-spiro-4'-piperidino)propyl]-10,11-dihydro-5H-dibenz [b,f]azepine (mosapramine), a new antipsychotic drug, were synthesized in order to determine their chemical structures. Pharmacological activities of the three main metabolites were compared with those of mosapramine. The activities of the metabolites were far less potent than those of mosapramine.
Tashiro
C
C
Research Laboratories, Yoshitomi Pharmaceutical Industries, Ltd., Fukuoka, Japan.
Yuasa
S
S
Fukuda
T
T
D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001058:Apomorphine / Q000037:antagonists & inhibitors; D001552:Benzazepines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D004285:Dogs; D066298:In Vitro Techniques; D007928:Lethal Dose 50; D008124:Locomotion / Q000187:drug effects; D008297:Male; D051379:Mice; D051381:Rats; D011954:Receptors, Dopamine / Q000378:metabolism; D013329:Structure-Activity Relationship
D014150:Antipsychotic Agents; D001552:Benzazepines; D011954:Receptors, Dopamine; C046384:mosapramine; D001058:Apomorphine