Studies towards the next generation of antidepressants. Part 1: Indolylcyclohexylamines as potent serotonin reuptake inhibitors

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1885-8. doi: 10.1016/s0960-894x(01)00334-1.

Abstract

A series of indolylcyclohexylamines possessing potent and selective serotonin reuptake inhibition is reported. The most interesting compounds proved to have subnanomolar 5-HT transporter activity, and exhibited moderate 5-HT(1A) affinity.

MeSH terms

  • Animals
  • Antidepressive Agents / chemical synthesis
  • Antidepressive Agents / pharmacology*
  • CHO Cells
  • Carrier Proteins / drug effects*
  • Carrier Proteins / metabolism
  • Cricetinae
  • Cyclohexylamines / chemical synthesis
  • Cyclohexylamines / pharmacology*
  • Humans
  • Indoles / chemistry
  • Inhibitory Concentration 50
  • Membrane Glycoproteins / drug effects*
  • Membrane Glycoproteins / metabolism
  • Membrane Transport Proteins*
  • Nerve Tissue Proteins*
  • Rats
  • Receptors, Adrenergic, alpha / drug effects*
  • Receptors, Adrenergic, alpha / metabolism
  • Receptors, Serotonin / drug effects*
  • Receptors, Serotonin / metabolism
  • Receptors, Serotonin, 5-HT1
  • Selective Serotonin Reuptake Inhibitors / metabolism
  • Selective Serotonin Reuptake Inhibitors / pharmacology*
  • Serotonin Plasma Membrane Transport Proteins
  • Structure-Activity Relationship

Substances

  • Antidepressive Agents
  • Carrier Proteins
  • Cyclohexylamines
  • Indoles
  • Membrane Glycoproteins
  • Membrane Transport Proteins
  • Nerve Tissue Proteins
  • Receptors, Adrenergic, alpha
  • Receptors, Serotonin
  • Receptors, Serotonin, 5-HT1
  • SLC6A4 protein, human
  • Serotonin Plasma Membrane Transport Proteins
  • Serotonin Uptake Inhibitors
  • Slc6a4 protein, rat