Chemistry, Pharmacology, and Behavioral Studies Identify Chiral Cyclopropanes as Selective α4β2-Nicotinic Acetylcholine Receptor Partial Agonists Exhibiting an Antidepressant Profile. Part II

A 3-pyridyl ether scaffold bearing a cyclopropane-containing side chain was recently identified in our efforts to create novel antidepressants that act as partial agonists at α4β2-nicotinic acetylcholine receptors. In this study, a systematic structure–activity relationship investigation was carried...

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Veröffentlicht in:	Journal of medicinal chemistry 2013-07, Vol.56 (13), p.5495-5504
Hauptverfasser:	Zhang, Han-Kun, Yu, Li-Fang, Eaton, J. Brek, Whiteaker, Paul, Onajole, Oluseye K, Hanania, Taleen, Brunner, Daniela, Lukas, Ronald J, Kozikowski, Alan P
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antidepressive Agents - chemistry Antidepressive Agents - pharmacology Binding, Competitive Caco-2 Cells Cell Line Cell Line, Tumor Cyclopropanes - chemistry Cyclopropanes - metabolism Cyclopropanes - pharmacology Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Enzyme System - metabolism Drug Stability Humans Male Mice Mice, Inbred BALB C Microsomes, Liver - drug effects Microsomes, Liver - enzymology Microsomes, Liver - metabolism Models, Chemical Molecular Structure Motor Activity - drug effects Nicotinic Agonists - chemistry Nicotinic Agonists - pharmacology Radioligand Assay Rats Receptors, Nicotinic - metabolism Stereoisomerism Structure-Activity Relationship Swimming - psychology
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