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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
2003-3-19
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pubmed:abstractText |
The synthesis of epibatidine derivatives modified at the 2-position of the pyridine or pyrimidine rings by reactive functions are described for potential irreversible site-directed coupling reactions on cysteine mutants of neuronal nicotinic acetylcholine receptors. An improved synthesis of the 7-azabicyclo[2,2,1]hepta-2,5-diene key intermediate has been developed to allow reproducible syntheses of the epibatidine derivatives. Binding tests and electrophysiological experiments allowed to select the 2-substituted alpha-chloroacetamido 13 and the chloropyrimidine derivative 11 as potential site-directed probes for the epibatidine binding site.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0960-894X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
24
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pubmed:volume |
13
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1001-4
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pubmed:dateRevised |
2005-11-17
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pubmed:meshHeading |
pubmed-meshheading:12643898-Animals,
pubmed-meshheading:12643898-Bicyclo Compounds, Heterocyclic,
pubmed-meshheading:12643898-Brain Chemistry,
pubmed-meshheading:12643898-Cell Line,
pubmed-meshheading:12643898-Cysteine,
pubmed-meshheading:12643898-Membrane Potentials,
pubmed-meshheading:12643898-Mutagenesis, Site-Directed,
pubmed-meshheading:12643898-Mutation,
pubmed-meshheading:12643898-Neurons,
pubmed-meshheading:12643898-Nicotinic Agonists,
pubmed-meshheading:12643898-Pyridines,
pubmed-meshheading:12643898-Pyrimidines,
pubmed-meshheading:12643898-Rats,
pubmed-meshheading:12643898-Receptors, Nicotinic,
pubmed-meshheading:12643898-Recombinant Fusion Proteins
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pubmed:year |
2003
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pubmed:articleTitle |
Syntheses and biological properties of cysteine-reactive epibatidine derivatives.
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pubmed:affiliation |
Laboratoire de Chimie Bioorganique, UMR 7514 CNRS, Faculté de Pharmacie, Université Louis Pasteur Strasbourg BP 24, 67401 Illkirch, cedex France.
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pubmed:publicationType |
Journal Article
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