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  • Discovery of dopamine D₄ receptor antagonists with planar chirality
    Sanna, Fabrizio ...
    Employing the D4 selective phenylpiperazine 2 as a lead compound, planar chiral analogs with paracyclophane substructure were synthesized and evaluated for their ability to bind and activate dopamine ... receptors. The study revealed that the introduction of a [2.2]paracyclophane moiety is tolerated by dopamine receptors of the D2 family. Subtype selectivity for D4 and ligand efficacy depend on the absolute configuration of the test compounds. Whereas the achiral single-layered lead 2 and the double-layered paracyclophane (R)-3 showed partial agonist properties, the enantiomer (S)-3 behaved as a neutral antagonist.
    Vir: Bioorganic & Medicinal Chemistry. - ISSN 0968-0896 (Vol. 21, no. 7, 2013, str. 1680-1684)
    Vrsta gradiva - članek, sestavni del ; neleposlovje za odrasle
    Leto - 2013
    Jezik - angleški
    COBISS.SI-ID - 120764163
    DOI

vir: Bioorganic & Medicinal Chemistry. - ISSN 0968-0896 (Vol. 21, no. 7, 2013, str. 1680-1684)

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