doi: 10.1016/j.bmcl.2007.12.075. Epub 2008 Jan 26.
Preparation and affinity profile of novel nicotinic ligands
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- PMID:18262785
- DOI: 10.1016/j.bmcl.2007.12.075
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Preparation and affinity profile of novel nicotinic ligands
Yves Charton et al. Bioorg Med Chem Lett..
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Abstract
Novel nicotinic ligands, characterized by the presence of an amino substituted cyclopropane ring connected to a pyridine nucleus, are described. Pharmacological investigation revealed that these compounds exhibit highest affinity for the rat alpha4beta2 subtype of the nicotinic receptor with no affinity for the muscarinic receptor. No appreciable affinity for the muscular or for the ganglionic nicotinic receptor was observed at concentrations up to 10 microM. The increase in cortical ACh release as well as a positive effect on memory in a social recognition test in rat are exemplified.
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