Synthesis, radiofluorination and pharmacological evaluation of a fluoromethyl spirocyclic PET tracer for central σ1 receptors and comparison with fluoroalkyl homologs

DOI: 10.1016/j.bmc.2011.11.002

Source and publish data:

Bioorganic and Medicinal Chemistry p. 257 - 269 (2012)

Update date:2022-09-26

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Authors:

Maisonial, Aurélie

Gro?e Maestrup, Eva

Wiese, Christian

Hiller, Achim

Schepmann, Dirk

Fischer, Steffen

Deuther-Conrad, Winnie

Steinbach, J?rg

Brust, Peter

Wünsch, Bernhard

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Article abstract of DOI:10.1016/j.bmc.2011.11.002

The spirocyclic σ₁ receptor ligand 1 (1′-benzyl-3- (fluoromethyl)-3H-spiro[[2]benzofuran-1,4′-piperidine]) was prepared in four steps starting from methoxy derivative 5. Due to its high σ₁ affinity (K_i = 0.74 nM) and selec

Full text of DOI:10.1016/j.bmc.2011.11.002

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