YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
医薬品の両性イオン化(第1報)4-(2-Chlorodibenz[b, f][1,4]oxazepin-11-yl)piaerazine, 4-(2-Chlorodibenzo[b, f][1,4]thiazepin-11-yl)-piperazine及び4-(11H-Dibenz[b, e]azepin-6-yl)piperazineのN-アルキルカルボン酸誘導体の合成とその薬理作用
村松 広美澤西 啓之岩崎 信彦垣内 正人大橋 徹生加藤 日出男伊藤 安夫
著者情報
ジャーナル フリー

1992 年 112 巻 7 号 p. 479-488

詳細
抄録

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.

著者関連情報
© by the PHARMACEUTICAL SOCIETY OF JAPAN
前の記事 次の記事
feedback
Top