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  • Title: Oxo-bridged isomers of aza-trishomocubane sigma (sigma) receptor ligands: Synthesis, in vitro binding, and molecular modeling.
    Author: Banister SD, Moussa IA, Jordan MJ, Coster MJ, Kassiou M.
    Journal: Bioorg Med Chem Lett; 2010 Jan 01; 20(1):145-8. PubMed ID: 19954972.
    Abstract:
    Isomeric oxo-bridged analogs of aza-trishomocubane sigma (sigma) receptor ligands were synthesized and shown to display a reduced affinity for the sigma receptor. In the case of phenethyl derivative 4, there was a concomitant introduction of high-affinity for the alpha(2C) adrenergic receptor, and moderate affinity for the dopamine transporter. Molecular modeling was undertaken to rationalize these results.
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