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    From a4ß2 Nicotinic Ligands to the Discovery of σ1 Receptor Ligands: Pharmacophore Analysis and Rational Design

    Access Status
    Fulltext not available
    Authors
    Yu, L.
    Zhang, H.
    Gunosewoyo, Hendra
    Kozikowski, A.
    Date
    2012
    Type
    Journal Article
    
    Metadata
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    Citation
    Yu, Li-Fang and Zhang, Han-Kun and Gunosewoyo, Hendra and Kozikowski, Alan P. 2012. From a4ß2 Nicotinic Ligands to the Discovery of σ1 Receptor Ligands: Pharmacophore Analysis and Rational Design. ACS Medicinal Chemistry Letters. 3 (12): pp. 1054-1058.
    Source Title
    ACS Medicinal Chemistry Letters
    DOI
    10.1021/ml3002715
    ISSN
    1948-5875
    URI
    http://hdl.handle.net/20.500.11937/17442
    Collection
    • Curtin Research Publications
    Abstract

    Comparative analyses of the pharmacophoric elements required for σ1 and nicotinic ligands led to the identification of a potent and selective σ1 ligand (15). Compound 15 displayed high selectivity for the σ1 receptor (Ki, σ1 = 4.1 nM; Ki, σ2 = 1312 nM) with moderate binding affinity for the DAT (Ki = 373 nM) and NET (Ki = 203 nM) in the PDSP broad screening panel of common CNS neurotransmitter transporters and receptors. The key finding in this present work is that a subtle structural modification could be used as a tool to switch a ligand’s selectivity between nAChRs and sigma receptors.

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