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Synthesis and in vitro evaluation of galanthamine derivatives for examination of nicotinic acetylcholine receptor system
Author(s) -
Schildan A.,
Schirrmacher R.,
Samochocki M.,
Christner C.,
Maelicke A.,
Rösch F.
Publication year - 2001
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.2580440186
Subject(s) - chemistry , nicotinic agonist , in vitro , acetylcholine receptor , acetylcholine , receptor , pharmacology , stereochemistry , nicotinic acetylcholine receptor , biochemistry , combinatorial chemistry , medicine
The syntheses and radioactive labeling of several galanthamine derivatives, 6‐O‐demethyl‐6‐O‐fluoroethylgalanthamine, 10‐N‐demethyl‐10‐N‐fluoroethylgalanthamine and N‐methylgalanthaminium are reported. First in vitro evaluations were carried out to determine their properties as allosterically potentiating ligands of nicotinic receptors. N‐methylgalanthaminium was found to be a promising candidate for further investigations.