Synthesis and NK1 receptor antagonistic activity of (+)-1-acyl-3-(3,4- dichlorophenyl)-3-[2-(spiro-substituted piperidin-1'-yl)ethyl]piperidines

Article abstract of DOI:10.1016/S0960-894X(98)00260-1

(±)-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.