Diazabicycloalkanesの研究(第2報)4-[β-(10-Phenothiazinyl)-ethyl]-1,4-diazabicyclo[4,4,0]-decaneおよび類似化合物の抗ヒスタミン作用ならびに向精神作用

概要

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The spasmolytic action on the contraction produced by histamine, acetylcholine, or barium, duration of antihistaminic activity, and some depressive activity on central nervous system were investigated on 4-[β-(10-phenothiazinyl)-ethyl]-1,4-diazabicyclo-[4,4,0]-decane (I) and its related compounds. The antihistaminic activity of I was found to be comparable to that of diphenhydramine and the duration of its action was more effective than the latter, though the antihistaminic activity of 2-chloro-I was very weak. In all cases of the tested compounds, the contraction produced by acetylcholine or barium was inhibited to a lesser degree. Both anticonvulsive action and depressive effect on spontaneous motor activity were weak and the potentiation of hypnosis was not observed. In accord with a general conclusion on phenothiazinylalkylamines, the most effective structural moiety of phenothiazinyl-diazabicyclodecanes for displaying of an antipsychotic activity was that possessing three carbon atoms between a basic diazabicyclodecane unit and a phenothiazine nucleus. When two carbon atoms were involved instead of three, effect on central nervous system was decreased and antihistaminic activity was enhanced.
公益社団法人日本薬学会の論文
1973-07-25