Differences in Brain 5-HT Transporter Dissociation Rates among Animal Species

Authors

  • Inge Erreboe,

    1. Department of Pharmacology, Laboratory of Neuropsychiatry, University of Copenhagen, Rigshospitalet-6102, DK-2100 Copenhagen Ø, Denmark
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  • Per Plenge,

    1. Department of Pharmacology, Laboratory of Neuropsychiatry, University of Copenhagen, Rigshospitalet-6102, DK-2100 Copenhagen Ø, Denmark
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  • Erling T. Mellerup

    1. Department of Pharmacology, Laboratory of Neuropsychiatry, University of Copenhagen, Rigshospitalet-6102, DK-2100 Copenhagen Ø, Denmark
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Author for correspondence: Per Plenge, Laboratory of Neuropsychiatry, Rigshospitalet-6102, Blegdamsvej 9, DK-2100 Ø Copenhagen, Denmark (fax (45) 31 39 35 46).

Abstract

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.

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