Differences in brain 5-HT transporter dissociation rates among animal species

Pharmacol Toxicol. 1995 Jun;76(6):376-9. doi: 10.1111/j.1600-0773.1995.tb00165.x.

Abstract

The potential of using receptor-ligand dissociation rates as a model for investigating molecular changes in receptors was tested using the dissociation of [3H]citalopram, [3H]paroxetine and [3H]imipramine from the brain 5-HT transporter of four different species (mouse, rat, pig and man). Since the dissociation rates of each of the three ligands differed in most of the species investigated, receptor-ligand dissociation rate constants would seem to be a sensitive measure of receptor conformation. The model could be useful in the search of structural variation in receptors whether attributable to genetic factors or to posttranslational modification.

Publication types

  • Comparative Study

MeSH terms

  • Adrenergic Uptake Inhibitors / pharmacology
  • Animals
  • Biological Transport, Active / drug effects
  • Brain Chemistry / drug effects*
  • Citalopram / pharmacology
  • Humans
  • Imipramine / pharmacology
  • Mice
  • Paroxetine / pharmacology
  • Rats
  • Serotonin / metabolism*
  • Serotonin Uptake Inhibitors / pharmacology
  • Swine

Substances

  • Adrenergic Uptake Inhibitors
  • Serotonin Uptake Inhibitors
  • Citalopram
  • Serotonin
  • Paroxetine
  • Imipramine