Differences in brain 5-HT transporter dissociation rates among animal species.
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.
D018759:Adrenergic Uptake Inhibitors / Q000494:pharmacology; D000818:Animals; D001693:Biological Transport, Active / Q000187:drug effects; D001923:Brain Chemistry / Q000187:drug effects*; D015283:Citalopram / Q000494:pharmacology; D006801:Humans; D007099:Imipramine / Q000494:pharmacology; D051379:Mice; D017374:Paroxetine / Q000494:pharmacology; D051381:Rats; D012701:Serotonin / Q000378:metabolism*; D017367:Selective Serotonin Reuptake Inhibitors / Q000494:pharmacology; D013552:Swine
D018759:Adrenergic Uptake Inhibitors; D015283:Citalopram; D007099:Imipramine; D017374:Paroxetine; D012701:Serotonin; D017367:Selective Serotonin Reuptake Inhibitors