Preparation and affinity profile of novel nicotinic ligands

…, C Guillonneau, B Lockhart, P Lestage…

Index: Charton, Yves; Guillonneau, Claude; Lockhart, Brian; Lestage, Pierre; Goldstein, Solo Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 6 p. 2188 - 2193

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Citation Number: 3

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 α4β2 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 10μM. The increase in ...