Uptake and release of 5-hydroxytryptamine by enteric 5-hydroxytryptaminergic neurones: effects of fluoxetine (Lilly 110140) and chlorimipramine

Br J Pharmacol. 1979 May;66(1):7-9. doi: 10.1111/j.1476-5381.1979.tb16089.x.


The effect of fluoxetine on uptake of 5-hydroxytryptamine (5-HT) by enteric 5-hydroxytryptaminergic neurones has been analyzed in order to compare further these neurones with 5-HT neurones of the CNS. In addition, the effects of fluoxetine and chlorimipramine on efflux of [3H]-5-HT from the myenteric plexus were also evaluated. Fluoxetine was found to be a competitive inhibitor of 5-HT uptake by the myenteric plexus and was a more potent inhibitor of 5-HT uptake than was chlorimipramine. However, chlorimipramine enhanced the efflux of [3H]-5-HT more than could be explained by inhibition of 5-HT uptake and, therefore, appears to have the additional action of releasing the amine. These observations, similar to those of others studying central neurones, support the view that enteric 5-HT neurones resemble those of the CNS and are a useful model for the evaluation of drugs.

MeSH terms

  • Animals
  • Clomipramine / pharmacology*
  • Dibenzazepines / pharmacology*
  • Fluoxetine / pharmacology*
  • Guinea Pigs
  • Half-Life
  • Kinetics
  • Male
  • Myenteric Plexus / drug effects
  • Myenteric Plexus / metabolism*
  • Neurons / drug effects
  • Neurons / metabolism*
  • Propylamines / pharmacology*
  • Serotonin / metabolism*


  • Dibenzazepines
  • Propylamines
  • Fluoxetine
  • Serotonin
  • Clomipramine