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  • Title: The potent 5-HT3 receptor antagonist (R)-zacopride labels an additional high affinity site in the central nervous system.
    Author: Kidd E, Bouchelet de Vendegies I, Levy JC, Hamon M, Gozlan H.
    Journal: Eur J Pharmacol; 1992 Jan 28; 211(1):133-6. PubMed ID: 1618262.
    Abstract:
    The binding characteristics of [3H](R)- and [3H](S)-zacopride were investigated in membranes from the rat entorhinal cortex and NG 108-15 clonal cells. In contrast to [3H](S)-zacopride which bound solely to 5-HT3 receptors, [3H](R)-zacopride recognized another class of binding sites, called the (R)-sites, in both membrane preparations. In addition to (R)-zacopride (Ki = 3-11 nM), only (R)-iodo-zacopride, (R)-dechloro-zacopride, prazosin and mianserin exhibited high to moderate affinity for the (R)-sites, whose possible functions remain to be established.
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