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Neuronal nAChR stereoselectivity to non‐natural epibatidine derivatives
Author(s) -
Bertrand Sonia,
Patt Jörg T,
Spang Jörg E,
Westera Gerrit,
Schubiger P.August,
Bertrand Daniel
Publication year - 1999
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/s0014-5793(99)00473-1
Subject(s) - epibatidine , nicotinic agonist , chemistry , acetylcholine receptor , nicotinic acetylcholine receptor , receptor , in vivo , acetylcholine , stereoselectivity , positron emission tomography , neuroscience , pharmacology , biophysics , stereochemistry , biochemistry , biology , microbiology and biotechnology , catalysis
The frog toxin epibatidine is one of the most powerful ligands of the neuronal nicotinic receptors and derivatives show promising possibilities for labeling in positron emission tomography studies. In an attempt to reduce epibatidine toxicity, new methyl derivatives were synthesized, tested in positron emission tomography imaging and in electrophysiology. labeling as well as physiological experiments highlighted the differences in sensitivity of the neuronal nicotinic acetylcholine receptors between two methyl enantiomers and the reduction in sensitivity caused by introducing the methyl group. At present, epibatidine derivatives seem the most promising compounds for in vivo labeling of neuronal nicotinic acetylcholine receptors.