387845-56-9Relevant academic research and scientific papers
Preparation and affinity profile of novel nicotinic ligands
Charton, Yves,Guillonneau, Claude,Lockhart, Brian,Lestage, Pierre,Goldstein, Solo
, p. 2188 - 2193 (2008/12/22)
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 10 μM. The increase in cortical ACh release as well as a positive effect on memory in a social recognition test in rat are exemplified.
1,1- and 1,2-disubstituted cyclopropane compounds
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, (2008/06/13)
A compound selected from those of formula (I): wherein: p represents an integer of from 0 to 6 inclusive, n represents an integer of from 0 to 6 inclusive, R1, and R2 represent a group selected from hydrogen, alkyl, aryl and arylalkyl, or R1+R2 form together with nitrogen carrying them saturated, monocyclic, or bicyclic system, X represents a group selected from oxygen, sulphur, a group —CH═CH—, methylene, a group of formula —HC═N—O— and a group of formula —O—CH2—CH═CH—, in which groups oxygen is linked to Y of the compounds of formula (I), Y represents a group selected from aryl, heteroaryl, arylalkyl, heteroarylalkyl, —C(O)—A, and —C(S)—A, A represents a group selected from alkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, and NR3R4 wherein R3, and R4 represent a group selected from hydrogen, alkyl, aryl, and arylalkyl, or R3+R4 form together with nitrogen carrying them monocyclic, or bicyclic (C3-C10) system, its isomers and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific nicotinic ligand of (α4β2 receptors.
