Author/Authors :
Hirokazu Kubota، نويسنده , , Yoshinori Okamoto، نويسنده , , Masahiro Fujii، نويسنده , , Ken Ikeda، نويسنده , , Makoto Takeuchi، نويسنده , , Tadao Shibanuma، نويسنده , , Yasuo Isomura، نويسنده ,
Abstract :
(±)-1-Acyl-3-(3,4-dichlorophenyl)-3-[2-(spiro-substituted piperidin-1′-yl)ethyl]piperidines and their quaternary ammonium salts were prepared and evaluated for their NK1 receptor antagonistic activity. Some of these inhibited SP-induced contraction in guinea pig ileum with IC50 values at a level of 10−9 M and showed potent inhibitory activity against selective NK1 receptor agonist-induced bronchoconstriction in guinea pigs.