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- W2080596570 abstract "A series of various N-substituted 3-(3-fluoropropyl)-3H-spiro[[2]benzofuran-1,4′-piperidines] (7) has been synthesized. In receptor binding studies, the N-benzyl derivative 7a (WMS-1813) revealed extraordinarily high σ1 receptor affinity (Ki = 1.4 nM) and excellent σ1/σ2 selectivity (>600fold). In vitro biotransformation of 7a with rat liver microsomes led to three main metabolites. N-Debenzylation was inhibited by introduction of an N-phenylethyl residue (7g). The PET tracer [18F]7a was synthesized by nucleophilic substitution of the tosylate 13 with K[18F]F-K222-carbonate complex. The decay corrected radiochemical yield of [18F]7a was 35−48% with a radiochemical purity of >99.5% and a specific activity of 150−238 GBq/μmol. The radiotracer properties were evaluated in female CD-1 mice by organ distribution and ex vivo brain autoradiography. The radiotracer uptake in the brain was fast and sufficient, with values of ∼4% injected dose per gram. Target specificity of [18F]7a was validated in blocking studies by preapplication of haloperidol, and significant reduction in the uptake of radioactivity was observed in the brain and peripheral organs expressing σ1 receptors." @default.
- W2080596570 created "2016-06-24" @default.
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- W2080596570 date "2009-09-11" @default.
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- W2080596570 title "Evaluation of Spirocyclic 3-(3-Fluoropropyl)-2-benzofurans as σ<sub>1</sub> Receptor Ligands for Neuroimaging with Positron Emission Tomography" @default.
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- W2080596570 doi "https://doi.org/10.1021/jm900909e" @default.
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