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  • Title: 18F-Labeled indole-based analogs as highly selective radioligands for imaging sigma-2 receptors in the brain.
    Author: Wang L, Ye J, He Y, Deuther-Conrad W, Zhang J, Zhang X, Cui M, Steinbach J, Huang Y, Brust P, Jia H.
    Journal: Bioorg Med Chem; 2017 Jul 15; 25(14):3792-3802. PubMed ID: 28549890.
    Abstract:
    We have designed and synthesized a series of indole-based σ2 receptor ligands containing 5,6-dimethoxyisoindoline or 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline as pharmacophore. In vitro competition binding assays showed that all ten ligands possessed low nanomolar affinity (Ki=1.79-5.23nM) for σ2 receptors and high subtype selectivity (Ki (σ2)/Ki (σ1)=56-708). Moreover, they showed high selectivity for σ2 receptor over the vesicular acetylcholine transporter (>1000-fold). The corresponding radiotracers [18F]16 and [18F]21 were prepared by an efficient one-pot, two-step reaction sequence with a home-made automated synthesis module, with 10-15% radiochemical yield and radiochemical purity of >99%. Both radiotracers showed high brain uptake and σ2 receptor binding specificity in mice.
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