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

Bioorg Med Chem Lett. 1998 Jun 16;8(12):1541-6. doi: 10.1016/s0960-894x(98)00260-1.

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.

MeSH terms

  • Animals
  • Bronchoconstriction / drug effects
  • Guinea Pigs
  • Ileum / drug effects
  • Ileum / physiology
  • Muscle Contraction / drug effects
  • Neurokinin-1 Receptor Antagonists*
  • Piperidines / chemical synthesis*
  • Piperidines / chemistry
  • Piperidines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Neurokinin-1 Receptor Antagonists
  • Piperidines