Synthesis and pharmacological evaluation of fluorinated benzo[7]annulen‐7‐amines as GluN2B‐selective NMDA receptor antagonists | Zendy

Thum Simone | Zendy; Schepmann Dirk | Zendy; Reinoso Raquel F. | Zendy; Alvarez Inés | Zendy; Ametamey Simon M. | Zendy; Wünsch Bernhard | Zendy

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Synthesis and pharmacological evaluation of fluorinated benzo[7]annulen‐7‐amines as GluN2B‐selective NMDA receptor antagonists

Author(s) -

Thum Simone,

Schepmann Dirk,

Reinoso Raquel F.,

Alvarez Inés,

Ametamey Simon M.,

Wünsch Bernhard

Publication year - 2019

Publication title -

journal of labelled compounds and radiopharmaceuticals

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.432

H-Index - 47

eISSN - 1099-1344

pISSN - 0362-4803

DOI - 10.1002/jlcr.3718

Subject(s) - chemistry , norepinephrine transporter , herg , selectivity , nmda receptor , stereochemistry , transporter , pharmacology , serotonin , receptor , biochemistry , biophysics , potassium channel , medicine , gene , biology , catalysis

Because of their neuroprotective potential, GluN2B‐selective ligands are of great interest for the treatment of various neurological and neurodegenerative disorders. Fluorinated benzo[7]annulen‐7‐amines, capable for PET, were synthesized by combining fluorinated phenylalkylamines with differently substituted ketones. Relationships between substitution pattern and GluN2B affinity as well as selectivity towards σ 1 and σ 2 receptors were investigated. Two promising ligands ( 18a and 20c ) were selected for further pharmacological evaluation. Besides a slight serotonin transporter (SERT), norepinephrine transporter (NET), and hERG affinity, they did not show interaction with other targets. Furthermore, the p K a value of a set fluorinated ligands, bearing the fluorine atom in different positions, was determined.

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