4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists II

Bioorg Med Chem Lett. 2002 Jul 8;12(13):1759-62. doi: 10.1016/s0960-894x(02)00250-0.

Abstract

A series of novel 4,4-disubstituted cyclohexylamines as NK(1) receptor antagonists is described: modifications to the amine moiety retain NK(1) receptor binding affinity whilst disrupting I(Kr) affinity.

MeSH terms

  • Amines / chemistry
  • Animals
  • Benzopyrans / chemistry
  • Binding Sites
  • CHO Cells
  • Cation Transport Proteins*
  • Clone Cells
  • Cricetinae
  • Cyclohexylamines / chemical synthesis*
  • Cyclohexylamines / pharmacokinetics
  • Cyclohexylamines / pharmacology*
  • Ether-A-Go-Go Potassium Channels
  • Gerbillinae
  • Inhibitory Concentration 50
  • Models, Molecular
  • Molecular Conformation
  • Neurokinin-1 Receptor Antagonists*
  • Piperidines / chemistry
  • Potassium Channels / drug effects
  • Potassium Channels / metabolism
  • Potassium Channels, Voltage-Gated*
  • Radioligand Assay
  • Receptors, Neurokinin-1 / chemistry
  • Receptors, Neurokinin-1 / drug effects
  • Structure-Activity Relationship
  • Time Factors

Substances

  • Amines
  • Benzopyrans
  • Cation Transport Proteins
  • Cyclohexylamines
  • Ether-A-Go-Go Potassium Channels
  • KCNH6 protein, human
  • Neurokinin-1 Receptor Antagonists
  • Piperidines
  • Potassium Channels
  • Potassium Channels, Voltage-Gated
  • Receptors, Neurokinin-1
  • L 706000