Affinities of fluoxetine, its enantiomers, and other inhibitors of serotonin uptake for subtypes of serotonin receptors

Neuropsychopharmacology. 1991 Aug;5(1):43-7.


The new antidepressant drugs, fluoxetine (and its enantiomers), citalopram, indalpine, paroxetine, and femoxetine show relatively weak affinities for 5-HT receptors as measured by radioligand binding to 5-HT-1(A,B,C and D), 5-HT-2, and 5-HT-3 subtypes. Fluoxetine and R(-)-fluoxetine, at near micromolar concentrations, inhibit 3H-mesulergine binding to 5-HT-1C receptors in bovine choroid plexus, and the R(-) enantiomer is 23 times more potent than the S(+) enantiomer. However, the near nanomolar potencies of these drugs as inhibitors of 5-HT uptake most likely account for their pharmacologic effects in animals.

MeSH terms

  • Animals
  • Antidepressive Agents / metabolism
  • Binding, Competitive / drug effects
  • Cattle
  • Choroid Plexus / drug effects
  • Choroid Plexus / metabolism
  • Ergolines / metabolism
  • Fluoxetine / metabolism*
  • In Vitro Techniques
  • Male
  • Radioligand Assay
  • Rats
  • Rats, Inbred Strains
  • Receptors, Serotonin / drug effects
  • Receptors, Serotonin / metabolism*
  • Serotonin / metabolism*
  • Serotonin Antagonists / pharmacology*
  • Stereoisomerism
  • Synaptosomes / drug effects
  • Synaptosomes / metabolism


  • Antidepressive Agents
  • Ergolines
  • Receptors, Serotonin
  • Serotonin Antagonists
  • Fluoxetine
  • Serotonin
  • mesulergine