1992 年 112 巻 7 号 p. 479-488
The piperazine N-alkylcarboxylic acids of 2-chlorodibenz[b, f] [1, 4] oxazepine (3a), 2-chlorodibenzo[b, f] [1, 4] thiazerine (3b), and dipenz[b, e]azepine (3c) from the corresponding piperazines (1a-c, R1=H) were synthesized via the piperazine N-alkylcarboxylates (2a-c). The pharmacolosical activities of the piperazine N-alkylcarboxylic acids (3a-c) were evaluated. Compared with the parent compounds (1a-c), 3a-c (n=1-5) showed weak inhibitory activities on the uptake of noradrenaline and 5-hydroxytryptamine (5-HT) into hypothalamus vesicles and moderate antagonistic actions to 5-HT2 and H1 in several tissues.